ÿþ<html xmlns:v="urn:schemas-microsoft-com:vml" xmlns:o="urn:schemas-microsoft-com:office:office" xmlns:w="urn:schemas-microsoft-com:office:word" xmlns:st1="urn:schemas-microsoft-com:office:smarttags" xmlns="http://www.w3.org/TR/REC-html40" xmlns:ns0="urn:schemas-microsoft-com:office:smarttags"> <head> <meta http-equiv=Content-Type content="text/html; charset=unicode"> <meta name=ProgId content=Word.Document> <meta name=Generator content="Microsoft Word 11"> <meta name=Originator content="Microsoft Word 11"> <link rel=File-List href="index_files/filelist.xml"> <link rel=Edit-Time-Data href="index_files/editdata.mso"> <link rel=OLE-Object-Data href="index_files/oledata.mso"> <!--[if !mso]> <style> v\:* {behavior:url(#default#VML);} o\:* {behavior:url(#default#VML);} w\:* {behavior:url(#default#VML);} .shape {behavior:url(#default#VML);} </style> <![endif]--> <title> </title> <o:SmartTagType namespaceuri="urn:schemas-microsoft-com:office:smarttags" name="City"/> <o:SmartTagType namespaceuri="urn:schemas-microsoft-com:office:smarttags" name="place"/> <o:SmartTagType namespaceuri="urn:schemas-microsoft-com:office:smarttags" name="PlaceType"/> <o:SmartTagType namespaceuri="urn:schemas-microsoft-com:office:smarttags" name="PlaceName"/> <!--[if gte mso 9]><xml> <o:DocumentProperties> <o:Author>prsbvlp</o:Author> <o:Template>Normal</o:Template> <o:LastAuthor>prsbvlp</o:LastAuthor> <o:Revision>20</o:Revision> <o:TotalTime>287</o:TotalTime> <o:Created>2012-04-10T11:38:00Z</o:Created> <o:LastSaved>2012-05-18T14:12:00Z</o:LastSaved> <o:Pages>5</o:Pages> <o:Words>9103</o:Words> <o:Characters>51892</o:Characters> <o:Company>University of Bath</o:Company> <o:Lines>432</o:Lines> <o:Paragraphs>121</o:Paragraphs> <o:CharactersWithSpaces>60874</o:CharactersWithSpaces> <o:Version>11.9999</o:Version> </o:DocumentProperties> </xml><![endif]--><!--[if gte mso 9]><xml> <w:WordDocument> <w:FormsDesign/> <w:ValidateAgainstSchemas/> <w:SaveIfXMLInvalid>false</w:SaveIfXMLInvalid> <w:IgnoreMixedContent>false</w:IgnoreMixedContent> <w:AlwaysShowPlaceholderText>false</w:AlwaysShowPlaceholderText> <w:BrowserLevel>MicrosoftInternetExplorer4</w:BrowserLevel> </w:WordDocument> </xml><![endif]--><!--[if gte mso 9]><xml> <w:LatentStyles DefLockedState="false" LatentStyleCount="156"> </w:LatentStyles> </xml><![endif]--><!--[if !mso]><object classid="clsid:38481807-CA0E-42D2-BF39-B33AF135CC4D" id=ieooui></object> <style> st1\:*{behavior:url(#ieooui) } </style> <![endif]--> <style> <!-- /* Font Definitions */ @font-face {font-family:Tahoma; 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background:white;mso-padding-alt:4.5pt 4.5pt 4.5pt 4.5pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes'> <td colspan=2 valign=top style='padding:4.5pt 4.5pt 4.5pt 4.5pt'> <table class=MsoNormalTable border=0 cellspacing=0 cellpadding=0 width="100%" style='width:100.0%;mso-cellspacing:0cm;mso-padding-alt:4.5pt 4.5pt 4.5pt 4.5pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes;mso-yfti-lastrow:yes'> <td width="13%" valign=top style='width:13.0%;padding:4.5pt 4.5pt 4.5pt 4.5pt'> <p class=MsoNormal><img width=150 height=196 id="_x0000_i1025" src=bvlp.gif></p> </td> <td width="49%" valign=top style='width:49.0%;padding:4.5pt 4.5pt 4.5pt 4.5pt'> <h3><span lang=DE style='font-size:20.0pt;mso-ansi-language:DE'>Professor B.V.L.Potter FMedSci<o:p></o:p></span></h3> <h6><span style='font-size:16.0pt'>Professor of Medicinal and Biological Chemistry<o:p></o:p></span></h6> <p><span style='font-size:14.0pt'>Telephone: (01225) 386639/ Fax (01225) 386114<br> E-mail: <a href="mailto:B.V.L.Potter@bath.ac.uk">B.V.L.Potter@bath.ac.uk</a><o:p></o:p></span></p> <p><span style='font-size:14.0pt'>Department of Pharmacy and Pharmacology<br> University of Bath (5 West - 3.3)<br> Claverton Down<br> Bath<br> BA2 7AY<br> <br> <strong>Visiting Professor of Medicinal Chemistry</strong><b><br> </b>University of Oxford (2006-2014)<br> <br> <b>Associate Member<br> </b>Dept of Pharmacology<br> University of Oxford, Mansfield Road, <br> Oxford OX1 3QT&nbsp;<br> </span>&nbsp;<o:p></o:p></p> </td> <td width="20%" valign=top style='width:20.0%;padding:4.5pt 4.5pt 4.5pt 4.5pt'> <p class=MsoNormal align=center style='text-align:center'><object classid="CLSID:D27CDB6E-AE6D-11CF-96B8-444553540000" id=DefaultOcxName width=500 height=374 codebase="http://download.macromedia.com/pub/shockwave/cabs/flash/swflash.cab#version=5,0,0,0"> <param name=movie value=docking.swf> <param name=quality value=high> <param name=bgcolor value="#FFFFFF"> <embed width="305" height="220" pluginspage="http://www.macromedia.com/shockwave/download/index.cgi?P1_Prod_Version=ShockwaveFlash" bgcolor="#FFFFFF" quality="high" type="application/x-shockwave-flash" src="docking.swf"></embed></object></p> <p><b><br> <br> </b>&nbsp;<br> <br> <br> &nbsp;&nbsp;</p> <table class=MsoNormalTable border=1 cellspacing=1 cellpadding=0 width=258 style='width:193.5pt;mso-cellspacing:.7pt;mso-padding-alt:0cm 5.4pt 0cm 5.4pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes;mso-yfti-lastrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=122 height=91 id="_x0000_i1027" src=Picture2.gif></p> </td> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=122 height=91 id="_x0000_i1028" src=Picture1.gif></p> </td> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=122 height=91 id="_x0000_i1029" src=Picture3.gif></p> </td> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=122 height=91 id="_x0000_i1030" src=Picture4.gif></p> </td> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=184 height=145 id="_x0000_i1031" src=ip3b.gif></p> </td> </tr> </table> <p class=MsoNormal><o:p></o:p></p> </td> </tr> </table> <p class=MsoNormal><o:p></o:p></p> </td> </tr> <tr style='mso-yfti-irow:1'> <td colspan=2 valign=top style='padding:4.5pt 4.5pt 4.5pt 4.5pt'> <h4><span style='font-size:16.0pt;color:red'><span style='mso-spacerun:yes'>                   </span><span style='mso-spacerun:yes'>                                                                                                                                                  </span></span><span style='font-size:20.0pt;color:red'>Biosketch&nbsp;&nbsp;<o:p></o:p></span></h4> <p><b style='mso-bidi-font-weight:normal'><span style='font-size:14.0pt'>&nbsp;Professor Potter studied chemistry as an Open Exhibitioner at <st1:place w:st="on"><st1:PlaceName w:st="on">Oxford</st1:PlaceName> <st1:PlaceType w:st="on">University</st1:PlaceType></st1:place>, graduating with first class honours and winning the Part II Thesis prize in Organic Chemistry. He completed his DPhil at Oxford in Bioorganic/Biological Chemistry as a Graduate Scholar and later Junior Research Fellow, working on the stereochemistry of enzyme-catalysed phosphoryl transfer reactions, developing the now textbook [<sup>16</sup>O,<sup>17</sup>O,<sup>18</sup>O] oxygen chiral phosphate ester approach that he applied to kinase, phosphatase and mutase enzyme mechanisms. After postdocs at Oxford and at the Max-Planck-Institute for Experimentelle Medizin in Goettingen, Germany, as Royal Society European Exchange Fellow and later Wissenschaftlicher Mitarbeiter der Max-Planck Gesellschaft, he became Lecturer in Biological Chemistry at Leicester University and won a Lister Institute of Preventive Medicine Fellowship. In 1990 he moved to the chair of Medicinal Chemistry at the University of Bath, as Lister Institute Research Professor where he holds the Established Chair in the Department of Pharmacy &amp; Pharmacology, as Head of the Medicinal Chemistry Section.<o:p></o:p></span></b></p> <p><b style='mso-bidi-font-weight:normal'><span style='font-size:14.0pt'>Fields of research activity are at the interface between Chemistry &amp; Biology and Chemistry &amp; Medicine ie Medicinal &amp; Biological Chemistry, Chemical Biology, Mechanistic Enzymology, Signal Transduction Chemistry, Anticancer Drug Design &amp; Discovery and Translational &amp; Molecular Medicine. [<a href="Cover%20Galleryrevised2.pdf">See Cover Gallery</a>]<span style='mso-spacerun:yes'>  </span>Particular interests are in the chemistry of cellular signalling, using carbohydrate, nucleotide and cyclitol chemistry to explore the chemical biology and pharmacology of second messengers that mobilise intracellular calcium, such as <em>myo</em>-inositol 1,4,5-trisphosphate (IP<sub>3</sub>) and the nucleotides cyclic ADP ribose (cADPR) and nicotinic acid adenine dinucleotide phosphate (NAADP). The research group is highly international [See <a href="GroupphotosF.pdf">Group Photo Gallery</a>]<span style='mso-spacerun:yes'>  </span>and has developed numerous synthetic structurally-modified ligands in all classes that have found widespread uses as chemical biological tools, some with proven activity in disease models. In Medicinal Chemistry, the group has pioneered inter alia, a novel pharmacophore in anti-cancer drug design and, unusually within an academic setting, has brought several compounds from novel therapeutic concept to multiple Phase I and II human clinical trials (19 to date), with other drug candidates in pre-clinical development. Evidence of efficacy has been notably in oncology directed against the novel<span style='mso-spacerun:yes'>  </span>target steroid sulfatase and in women s health. Non-steroidal cancer drugs designed at <st1:place w:st="on"><st1:City w:st="on">Bath</st1:City></st1:place> are currently in Phase II clinical trials in metastatic breast cancer, endometrial cancer &amp;<span style='mso-spacerun:yes'>  </span>prostate cancer<span style='mso-spacerun:yes'>  </span>and the steroid derivative PGL2001 is currently in Phase II trials for endometriosis.<o:p></o:p></span></b></p> <p class=MsoNormal>&nbsp;<b style='mso-bidi-font-weight:normal'><span style='font-size:14.0pt'>He co-founded the university spin out company <em>Sterix Ltd</em> where he was Director of Medicinal Chemistry and subsequently Chief Scientific Officer and that was acquired by major pharma; he is a Fellow of the Royal Society of Chemistry, the Society of Biology, the Institute of Directors and the Royal Society of Arts and has published over 475 research articles [see eg <span style='color:#4E4E4E'><a href="http://www.researcherid.com/rid/A-1845-2012">http://www.researcherid.com/rid/A-1845-2012</a></span>]with ca 400 formally granted patents to date worldwide from many diverse families, including 45 USPs, 25 EPs and 10 JPs. He was elected to Membership of the <em>Lister Institute of Preventive Medicine</em> in 1995. He served on the <i style='mso-bidi-font-style:normal'>BBSRC Intracellular Signalling Programme Committee</i> (1992 1996) and the <i style='mso-bidi-font-style:normal'>EPSRC Synthetic and Biological Chemistry College</i> (1995 1997). He is a member of the <i style='mso-bidi-font-style:normal'>Biochemical Society</i>, the <i style='mso-bidi-font-style:normal'>American Association for Cancer Research</i> and the <i style='mso-bidi-font-style:normal'>American Chemical Society</i> and was a committee member of the <i style='mso-bidi-font-style:normal'>Society for Medicines Research</i> (2002-2006). He was a member of the <i style='mso-bidi-font-style:normal'>HEFCE Pharmacy/ Pharmacology Panel</i> for the RAE2001 and RAE2008 exercises and the <i style='mso-bidi-font-style:normal'>Research Excellence Framework (REF) Expert Group Panel</i> 2009 and was a member of the <em>Molecules, Genes &amp; Cells </em><i style='mso-bidi-font-style:normal'>Funding Panel<em> </em></i>of the Wellcome Trust (2006-2011). He is on the editorial boards of the ACS <em>Journal of Medicinal Chemistry</em>, AACR <em>Molecular Cancer Therapeutics</em>, <i style='mso-bidi-font-style:normal'>Messenger</i>, <em>Perspectives in Medicinal Chemistry</em> and <em>Future Medicinal Chemistry</em>, has served on the boards of the <em>Biochemical Journal</em>, <em>Carbohydrate Research</em>, <em>Current Organic Synthesis</em>, <em>Drug Design &amp; Discovery </em>and is currently Associate Editor of the <em>Journal of Steroid Biochemistry &amp; Molecular Biology </em>and Editor of the <em>Biochemical Journal's BJChemBio</em>. He received a DSc from <st1:City w:st="on">Oxford</st1:City> in 1993 and is Visiting Professor of Medicinal Chemistry at <st1:PlaceName w:st="on">Oxford</st1:PlaceName> <st1:PlaceType w:st="on">University</st1:PlaceType> and Associate Member, Department of Pharmacology, <st1:place w:st="on"><st1:City w:st="on">Oxford</st1:City></st1:place>. He is named in the  <a href="H-index%20ranking%20of%20living%20chemists(March%202011)_tcm18-85867.pdf">H-index ranking of living chemists</a> listing (H-index 55).<span style='color:#4E4E4E'><o:p></o:p></span></span></b></p> <p><b style='mso-bidi-font-weight:normal'><span style='font-size:14.0pt'>Professor Potter was the recipient of the Royal Society of Chemistry UCB-Celltech Industrially Sponsored Award and Medal for Chemical Biology for 2007, the Royal Society of Chemistry George and Christine Sosnovsky Award &amp; Medal for Cancer Medicinal Chemistry for 2007/8 with an RSC Endowed Lectureship, the Royal Society of Chemistry Biological &amp; Medicinal Chemistry Sector s Malcolm Campbell Memorial Prize &amp; Medal for 2009, the GlaxoSmithKline International Achievement Award for 2009 and the Royal Society of Chemistry Interdisciplinary Prize &amp; Medal for 2010 with an RSC Endowed Lectureship. He was elected to Fellowship of the <st1:place w:st="on"><st1:PlaceType w:st="on"><em>Academy</em></st1:PlaceType><em> of <st1:PlaceName w:st="on">Medical Sciences</st1:PlaceName></em></st1:place><em> </em>in 2008 and in 2009 to Membership of the <em>Academia Europaea</em>.</span></b>&nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:2;height:129.55pt'> <td style='padding:4.5pt 4.5pt 4.5pt 4.5pt;height:129.55pt'> <p align=center style='text-align:center'><b><span style='font-size:14.0pt; color:red'>X-ray crystal structures of synthetic ligands from the group determined in complex with their target proteins:<o:p></o:p></span></b></p> <p align=center style='text-align:center'><b><span style='font-size:14.0pt; color:red'><o:p>&nbsp;</o:p></span></b></p> <div align=center> <table class=MsoNormalTable border=1 cellpadding=0 width="90%" style='width:90.0%;mso-cellspacing:1.5pt;mso-padding-alt:0cm 5.4pt 0cm 5.4pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal>&nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:1'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=272 height=261 id="_x0000_i1677" src=BP1.jpg></p> </td> </tr> <tr style='mso-yfti-irow:2'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal>&nbsp;<br> &nbsp;&nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:3'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=264 height=250 id="_x0000_i1678" src="pic2_.jpg" alt="pic2_.jpg"></p> </td> </tr> <tr style='mso-yfti-irow:4'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:5'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=219 height=208 id="_x0000_i1679" src=pic3.jpg></p> </td> </tr> <tr style='mso-yfti-irow:6'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:7'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=219 height=186 id="_x0000_i1680" src=pic12.jpg alt=pic12></p> </td> </tr> <tr style='mso-yfti-irow:8'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:9'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=219 height=207 id="_x0000_i1681" src=pic4.jpg></p> </td> </tr> <tr style='mso-yfti-irow:10'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:11;mso-yfti-lastrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><img border=0 width=219 height=219 id="_x0000_i1833" src=pic5.jpg></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> <p class=MsoNormal><!--[if gte vml 1]><v:shapetype id="_x0000_t75" coordsize="21600,21600" o:spt="75" o:preferrelative="t" path="m@4@5l@4@11@9@11@9@5xe" filled="f" stroked="f"> <v:stroke joinstyle="miter"/> <v:formulas> <v:f eqn="if lineDrawn pixelLineWidth 0"/> <v:f eqn="sum @0 1 0"/> <v:f eqn="sum 0 0 @1"/> <v:f eqn="prod @2 1 2"/> <v:f eqn="prod @3 21600 pixelWidth"/> <v:f eqn="prod @3 21600 pixelHeight"/> <v:f eqn="sum @0 0 1"/> <v:f eqn="prod @6 1 2"/> <v:f eqn="prod @7 21600 pixelWidth"/> <v:f eqn="sum @8 21600 0"/> <v:f eqn="prod @7 21600 pixelHeight"/> <v:f eqn="sum @10 21600 0"/> </v:formulas> <v:path o:extrusionok="f" gradientshapeok="t" o:connecttype="rect"/> <o:lock v:ext="edit" aspectratio="t"/> </v:shapetype><v:shape id="_x0000_i1844" type="#_x0000_t75" style='width:155.25pt; height:183pt;mso-position-horizontal:absolute; mso-position-horizontal-relative:char;mso-position-vertical:absolute; mso-position-vertical-relative:line'> <v:imagedata src="index_files/image002.emz" o:title=""/> </v:shape><![endif]--><![if !vml]><img border=0 width=207 height=244 src="index_files/image003.gif" v:shapes="_x0000_i1844"><![endif]></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> <p class=MsoNormal><!--[if gte vml 1]><v:shape id="_x0000_i1845" type="#_x0000_t75" style='width:159pt;height:271.5pt;mso-position-horizontal:absolute; mso-position-horizontal-relative:char;mso-position-vertical:absolute; mso-position-vertical-relative:line'> <v:imagedata src="index_files/image004.png" o:title=""/> </v:shape><![endif]--><![if !vml]><img border=0 width=212 height=362 src="index_files/image005.gif" v:shapes="_x0000_i1845"><![endif]></p> <p class=MsoNormal><o:p>&nbsp;</o:p></p> </td> </tr> </table> </div> <p class=MsoNormal align=center style='text-align:center'><o:p>&nbsp;</o:p></p> <p class=MsoNormal align=center style='text-align:center'><o:p>&nbsp;</o:p></p> <p class=MsoNormal align=center style='text-align:center'><o:p>&nbsp;</o:p></p> <p class=MsoNormal align=center style='text-align:center'><b><o:p>&nbsp;</o:p></b></p> </td> <td style='padding:4.5pt 4.5pt 4.5pt 4.5pt;height:129.55pt'> <p align=center style='text-align:center'><b><span style='font-size:20.0pt; color:red'>Research&nbsp;Interests<strong><o:p></o:p></strong></span></b></p> <p><strong><span style='font-size:16.0pt;color:red'>Research is centred around four main areas of Chemical Biology and Synthetic Medicinal and Biological Chemistry:</span></strong><b><span style='font-size:16.0pt'><br> </span></b><span style='font-size:16.0pt'><br> All projects concern the design, synthesis and biological evaluation of active organic molecules at the interfaces of Chemistry &amp; Biology, ultimately aimed at the dissection of biological mechanisms through chemical biological intervention and molecular biology, or at the interface of Chemistry &amp; Medicine through intelligent drug design &amp; discovery with the aim of moving translationally from 'concept to clinic'. A unifying general biological theme is centred around cellular signalling processes and concerns both entities involved in endocrine signalling and their modulation in oncology and endocrinology, as well as signal transduction processes in particular, particularly those involving signalling through elevation of&nbsp;intracellular Ca<sup>2+</sup>. Work is underpinned by in house expression and purification of relevant proteins, biochemical assays, protein crystallography and by <i>in silico</i> computational design techniques as well as by synthetic chemistry. Where possible, synthesized ligands are co-crystallised with relevant binding proteins for structure-based design in both broad areas and examples of solved X-ray structures from the group are shown (left). The four main themes are:</span></p> <div> <p class=MsoNormal><strong><span style='font-size:16.0pt;color:red'>Inositol phosphate-mediated cellular signalling</span></strong><span style='font-size: 16.0pt;color:red'><br> </span><span style='font-size:16.0pt'>Research concerns the synthesis of novel probes and modulators primarily of the D-<em>myo</em>-inositol 1,4,5-trisphosphate second messenger pathway. Novel agonists, antagonists and enzyme inhibitors are being synthesised for chemical biological intervention using carbohydrate, cyclitol, nucleotide and phosphorus chemistry. The unusual activity of the <a href="Potter_JOC_guanophostin_published.pdf">very potent agonist Adenophostin A</a> has been a long term focus using total synthesis. <a href="JMCsureshanpublished.pdf">Recent work</a> has further refined our proposed model for interaction with the inositol trisphosphate receptor, showing that the long-thought <a href="chemcommsureshanfeb09published.pdf">vicinal bisphosphate motif is not necessary</a> for activity. Chemical biology tools designed at <st1:place w:st="on"><st1:City w:st="on">Bath</st1:City></st1:place> are illuminating the <a href="376%20-%20Rossi%20et%20al.pdf">inositol trisphosphate receptor machinery</a> using partial agonists. Intracellular Ca<sup>2+</sup> mobilising activity is evaluated in whole and permeabilised cells via a world-wide network of collaborators and often in collaboration with colleagues at <ns0:place><ns0:placename><st1:City w:st="on">Cambridge</st1:City></ns0:placename></ns0:place> <ns0:placetype><span style='mso-spacerun:yes'> </span>and <st1:place w:st="on"><st1:PlaceName w:st="on">Oxford</st1:PlaceName> <st1:PlaceType w:st="on">Universities</st1:PlaceType></st1:place></ns0:placetype>. Recent work is focusing upon higher inositol polyphosphates such as the pentakisphosphate, which is both antiproliferative and antiangiogenic<i style='mso-bidi-font-style:normal'> </i>and surprisingly enters cancer cells and blocks PKB/Akt signalling. Synthetic derivatives are <i style='mso-bidi-font-style: normal'>pro</i>-apoptopic, active in models of cancer and specifically inhibit 3-phosphoinositide protein kinase 1 (PDK1). Selected ligands and their surrogates are also co-crystallised with suitable binding proteins for X-ray crystallography and structure-based design; examples shown are a Bruton s tyrosine kinase-IP<sub>4 </sub>complex and a benzene polyphosphate <a href="Mills_-_Chemical_Biology_Paper_-_PUBLISHED.pdf">analogue co-crystallised with the PH domain of protein kinase B±.</a> They are also designed with added fluorophores for cellular imaging and single molecule applications in signalling.<span style='mso-spacerun:yes'>  </span>The group is working closely with the Structural Genomics Consortium in <ns0:city><ns0:place>Stockholm</ns0:place></ns0:city> on proteins that act on inositol phosphates and phospholipids and has been supported since 1995 by three Wellcome Trust Programme Grants. Together, we recently solved the first X-ray crystal structure of the important drug target SHIP2 in complex with a synthetic biphenyl-based lipid headgroup mimic that opens up a potential <a href="SHIP2%20paper2012published.pdf">new route for drug design</a>, involving movement of a <a href="Loop%20Dynamics.mpeg">flexible loop</a> close to the active site. We are also working with structural biology colleagues at the University of East Anglia on the <i style='mso-bidi-font-style:normal'>Arabidopsis </i>IPK1 kinase using our synthetic inositol polyphosphate surrogates.<o:p></o:p></span></p> </div> <p><strong><span style='font-size:16.0pt;color:red'>Cyclic ADP-ribose - a new second messenger</span></strong><span style='font-size:16.0pt;color:red'><br> </span><span style='font-size:16.0pt'>The cyclic nucleotide cyclic adenosine 5'-diphosphate ribose, formed via enzyme-mediated cyclisation of NAD<sup>+</sup> is a recently identified Ca<sup>2+</sup>-releasing second messenger, that works independently of inositol 1,4,5-trisphosphate. A combination of techniques <a href="Potter_JMC_2deoxycADPR_mar08_published.pdf">from total synthesis to chemo-enzymatic methods</a> is<span style='mso-spacerun:yes'>  </span>being used to synthesize novel mimics, agonists, antagonists and ADP-ribosyl cyclase inhibitors related to this new signalling pathway for chemical biological intervention in multiple systems, but especially in T cells, working in collaboration with colleagues at the <ns0:placetype><st1:PlaceType w:st="on">University</st1:PlaceType></ns0:placetype> of <ns0:placename><st1:PlaceName w:st="on">Hamburg</st1:PlaceName></ns0:placename> and <ns0:place><ns0:placename><st1:place w:st="on"><st1:PlaceName w:st="on">Oxford</st1:PlaceName></st1:place></ns0:placename></ns0:place> <ns0:placetype><st1:PlaceType w:st="on">University</st1:PlaceType></ns0:placetype>. Recent work has <a href="OBCcADPRJan2011published.pdf">defined SAR parameters for an invertebrate cADPR receptor</a> and also focused upon a total synthesis of a stable active macrocyclic template. [see <a href="CoverJOC2012.pdf">cover design</a>] Selected ligands are <a href="JBC2FNAD09published.pdf">co-crystallised with suitable binding proteins</a> such as ADP-ribosyl cyclases and CD38 for X-ray crystallography, structure-based design and elucidation of enzyme mechanisms; examples shown are a CD38-cIDPR complex and a complex of <em>Aplysia californica</em> ADP-ribosyl cyclase with 2-fluoro-NAD<sup>+</sup>. Recent work demonstrates the continuing unusual effects of <a href="JMCchristelle2012published.pdf">targeted chemical modification in an active but stable template</a> that we have pioneered. <o:p></o:p></span></p> <p><span style='font-size:16.0pt'><!--[if gte vml 1]><v:shape id="_x0000_i1846" type="#_x0000_t75" alt="" style='width:96pt;height:112.5pt; mso-position-horizontal:absolute;mso-position-horizontal-relative:char; mso-position-vertical:absolute;mso-position-vertical-relative:line'> <v:imagedata src="index_files/image006.gif" o:title="CD38-NAD"/> <o:lock v:ext="edit" cropping="t"/> </v:shape><![endif]--><![if !vml]><img border=0 width=128 height=150 src="index_files/image006.gif" v:shapes="_x0000_i1846"><![endif]><o:p></o:p></span></p> <p><strong><span style='font-size:16.0pt;color:red'>ADP-ribose, a new second messenger &amp; TRPM2</span><span style='color:red'><o:p></o:p></span></strong></p> <p><span style='font-size:16.0pt'>Adenosine 5'-diphosphoribose controls opening of the ligand-gated cation channel TRPM2, expressed mainly in the immune system and in the brain, by binding to the cytoplasmic C-terminal NudT9H domain. Small molecules are being designed, working also in collaboration with colleagues at <st1:place w:st="on"><st1:PlaceName w:st="on">Hamburg</st1:PlaceName> <st1:PlaceType w:st="on">University</st1:PlaceType></st1:place>, to interfere with the ADPR-TRPM2 interaction, that will elucidate structure-activity relationships and may be of potential therapeutic application.<o:p></o:p></span></p> <p><!--[if gte vml 1]><v:shape id="_x0000_i1847" type="#_x0000_t75" alt="File:Adenosine diphosphate ribose 3D.png" href="//upload.wikimedia.org/wikipedia/commons/0/02/Adenosine_diphosphate_ribose_3D.png" style='width:165.75pt;height:104.25pt;mso-position-horizontal:absolute; mso-position-horizontal-relative:char;mso-position-vertical:absolute; mso-position-vertical-relative:line' o:button="t" filled="t" fillcolor="#bbe0e3"> <v:fill o:detectmouseclick="t"/> <v:imagedata src="index_files/image011.png" o:title="800px-Adenosine_diphosphate_ribose_3D"/> </v:shape><![endif]--><![if !vml]><span style='mso-ignore:vglayout'><img border=0 width=221 height=139 src="index_files/image013.jpg" alt="File:Adenosine diphosphate ribose 3D.png" title="" v:shapes="_x0000_i1847"></span><![endif]></p> <p><span style='font-size:16.0pt'>This project is supported by a Wellcome Trust Project Grant.<o:p></o:p></span></p> <p><strong><span style='font-size:16.0pt;color:red'><u2:p></u2:p>NAADP - a new second messenger</span></strong><span style='font-size:16.0pt'><br> The NAD<sup>+</sup> derivative, nicotinic acid adenine dinucleotide phosphate (NAADP) is a Ca<sup>2+</sup>-releasing second messenger that works independently of inositol 1,4,5-triphosphate and cADPR. NAADP represents a newly identified messenger in T cells involved in antigen receptor-mediated calcium signalling.</span><span style='font-size:16.0pt;font-family:AdvP492F86; mso-bidi-font-family:AdvP492F86;color:#3333FF'> </span><span style='font-size:16.0pt'>A combination of techniques from total synthesis to chemo-enzymatic methods is being used to design and synthesize novel mimics, antagonists and chemical biological tools to probe this new signalling pathway, with colleagues at <ns0:state>Hamburg</ns0:state> and <ns0:city><ns0:place>Oxford</ns0:place></ns0:city>. We have shown in recent work that calcium signalling controlled by nicotinic acid adenine dinucleotide phosphate is relevant for the pathogenic potential of autoimmune effector T cells. Specific inhibition of the NAADP signalling pathway is emerging as a way to specifically and effectively modulate T-cell activation and has particular <a href="Potter-BRAINjul2010published.pdf">potential in the therapy of autoimmune diseases</a> such as multiple sclerosis and the first <a href="PNASpublished.pdf">small molecules can be designed</a> to illuminate such potential.<b> <o:p></o:p></b></span></p> <p><b><span style='font-size:16.0pt'><!--[if gte vml 1]><v:shape id="_x0000_i1848" type="#_x0000_t75" alt="" style='width:108pt;height:124.5pt; mso-position-horizontal:absolute;mso-position-horizontal-relative:char; mso-position-vertical:absolute;mso-position-vertical-relative:line'> <v:imagedata src="index_files/image007.gif" o:title="NAADP"/> <o:lock v:ext="edit" cropping="t"/> </v:shape><![endif]--><![if !vml]><img border=0 width=144 height=166 src="index_files/image007.gif" v:shapes="_x0000_i1848"><![endif]><o:p></o:p></span></b></p> <p><strong><span style='font-size:16.0pt;color:red'>Anticancer drug design, discovery &amp; translational medicine</span></strong><span style='font-size: 16.0pt;color:red'><o:p></o:p></span></p> <p><em><span style='font-size:16.0pt;color:blue'>Steroid Sulfatase Inhibitors</span></em><em><span style='font-size:16.0pt'>:</span></em><span style='font-size:16.0pt'><br> In this area, and working with colleagues at Imperial College London, we are pioneering a whole new area of drug research, based upon inhibition of steroid sulfatase (STS), and have discovered a unexplored drug pharmacophore supporting a novel therapeutic concept for postmenopausal women with hormone-dependent breast cancer. Many tumours are 17²-estradiol-dependent and hydrolysis of the conjugate estrone 3-<i style='mso-bidi-font-style:normal'>O</i>-sulfate by <ns0:stockticker>STS</ns0:stockticker> is a source of tumour estrogen, especially <i style='mso-bidi-font-style:normal'>in situ</i>. We designed the first highly potent active-site-directed time- and concentration-dependent irreversible inhibitors of STS. Enzyme sulfamoylation and inactivation occurs most likely via a liberated highly electrophilic sulfonylamine species. <a href="ChemMedChemSTSpublished.pdf">Recent work has consolidated the SAR</a> of this new drug class. Our early agent has reached multiple phase II clinical trials for a hormone replacement therapy indication. The virtual absence of hepatic estrogenicity and the production of clotting factors may reduce the risk of adverse events normally associated with HRT. Estrogen sulfamates are a new type of estrogen which not only inhibit STS, but are sequestered by carbonic anhydrase (CAII) </span><span lang=EN style='font-size:16.0pt; mso-ansi-language:EN'>in erythrocytes and transit the liver without undergoing first-pass inactivation. They </span><span style='font-size:16.0pt'>possess many attractive properties for drug design, being orally active with excellent bioavailability and pharmacokinetics and bound as their anion by CAII in red blood cells. We have solved the X-ray crystal structures of numerous<span style='mso-spacerun:yes'>  </span>sulfamate drug : CAII complexes at <ns0:place><ns0:city>Bath</ns0:city></ns0:place>.</span><span style='font-size:16.0pt;mso-ansi-language:EN-US'> </span><span style='font-size:16.0pt'>The movie above shows the docking of a biphenyl-based dual inhibitor, designed at <ns0:place><ns0:city>Bath</ns0:city></ns0:place>, into the active site of<span style='mso-spacerun:yes'>  </span>human CAII, based upon our X-ray crystal structure of the inhibitor-CAII complex.<o:p></o:p></span></p> <p class=MsoNormal style='mso-margin-top-alt:auto;mso-margin-bottom-alt:auto; text-align:justify'><span lang=EN-US style='font-size:16.0pt;mso-ansi-language: EN-US'><u2:p></u2:p>The STS inhibitor PGL2001, designed at <ns0:place><ns0:city><st1:place w:st="on"><st1:City w:st="on">Bath</st1:City></st1:place></ns0:city></ns0:place>,<span style='mso-spacerun:yes'>  </span>has the potential to be the first of a new class of drug for benign gynaecological conditions and entered Phase II clinical trial against endometriosis during 2012. </span><span lang=EN style='font-size:16.0pt;mso-ansi-language:EN'>O</span><span style='font-size: 16.0pt'>ur non-steroidal drug STX64 [6-oxo-6,7,8,9,10,11-hexahydrocyclo-hepta[c] [1]benzopyran-3-yl sulfamate], formally named <i style='mso-bidi-font-style:normal'>Irosustat</i>, a potent tricylic sulfamate derivative, was selected by CRUK for a  first-in-class clinical trial of a <ns0:stockticker>STS</ns0:stockticker> inhibitor in women with advanced breast cancer and showed evidence of stable disease.<i style='mso-bidi-font-style:normal'> </i>Phase II trials in patients are now complete in endometrial and breast cancer, and further trials have taken place in men in androgen-dependent prostate cancer. The drug class also has potential in ovarian cancer and in other hormone dependent pathologies.<o:p></o:p></span></p> <p><span style='font-size:16.0pt'><u2:p></u2:p>Aromatase inhibitors in current clinical use block the biosynthesis of steroidal estrogens by inhibiting aromatisation of the A-ring of androgenic precursors. We recently defined a novel class of <i style='mso-bidi-font-style:normal'>picomolar</i>-potent aromatase inhibitor based upon a biphenyl template linked to a triazole moiety. Using the topical idea of polypharmacology, blockade of aromatase and sulfatase enzymes should provide a more effective endocrine therapy.<span style='mso-spacerun:yes'>  </span>We proposed the concept of a <a href="CMCAromataseVorozole1423_ftp.pdf">dual aromatase-sulfatase inhibitor</a> in one molecule and introduced our aryl sulfamate pharmacophore into three clinically established aromatase inhibitors. Advanced dual inhibitors have great potential, being exquisitely potent with dual IC<sub>50</sub>s of eg 130pM and 18pM.<o:p></o:p></span></p> <p><u2:p><span style='font-size:16.0pt'>A steroidal antitumour/antiangiogenesis microtubule disruptor of clinical potential, using our new pharmacophore for dual structural augmentation and protection against metabolic conjugation, is in formal preclinical development for oncology. STX 140, suitable for targeting taxane resistant tumours, is active against multi-drug and taxane-resistant tumours and those expressing the drug efflux pump P-glycoprotein. </span><span lang=EN-US style='font-size:16.0pt;mso-ansi-language:EN-US;mso-fareast-language: JA;mso-bidi-font-weight:bold'>It surprisingly binds to carbonic anhydrase via the non-aryl sulfamate and we discovered by protein crystallography a second STX140 binding site on the enzyme</span><span style='font-size:16.0pt'>. The pharmacophoric elements of STX140 are being translated into highly potent <a href="ChemCommCover_x2x.pdf">chimeric non-steroidal microtubule disruptors</a> with very attractive pharmaceutical <a href="HighlightsChemBiolmay2010frontpage.pdf">properties and activities</a> and this template has considerable potential more widely as a <a href="ml200232c.pdf">steroidomimetic template</a> that is being actively pursued.<o:p></o:p></span></p> <p class=MsoNormal style='mso-margin-top-alt:auto;mso-margin-bottom-alt:auto; text-align:justify'><em><span style='font-size:16.0pt;color:blue'><u2:p></u2:p>Dehydrogenase Inhibition</span></em><strong><i><span style='font-size:16.0pt;color:blue'>:</span></i></strong><span style='font-size:16.0pt'> 17²-Hydroxysteroid dehydrogenases types 1&amp;3(17²-HSDs) catalyse the interconversion between the oxidised and reduced forms of androgens and estrogens at the 17-position, are expressed in malignant cells and possess unexploited therapeutic potential as targets for anticancer drug design. Potent and selective low nanomolar inhibitory druglike candidates are being synthesised and evaluated using both enzymes and via protein crystallography. Small molecule synthetic drug candidates directed at<span style='mso-spacerun:yes'>  </span>both 17²-HSD type 1 has successfully been demonstrated to exhibit <i style='mso-bidi-font-style:normal'>in vivo</i> activity in tumour models. Efforts directed at novel approaches to diabetes and metabolic syndrome are being pursued by <a href="CMCadamantylethanone1616_ftp.pdf">inhibition of the target</a> enzyme <a href="FMC11betapublished.pdf">11²-hydroxysteroid dehydrogenase</a>. Low <a href="CMCadamantylheterocyclic1439_ftp.pdf">nanomolar active inhibitors</a> have been designed, synthesized and evaluated in whole cell assays using human 11²-HSD transfected HEK293 cells and by protein crystallography. Research in these areas has been supported by CRUK and through industry.<o:p></o:p></span></p> <p class=MsoNormal style='mso-margin-top-alt:auto;mso-margin-bottom-alt:auto; text-align:justify'><strong><span style='font-size:16.0pt;color:red; mso-bidi-font-style:italic'>Novel antagonists at the nicotinic acetylcholine receptor </span><span style='color:red;mso-bidi-font-style:italic'><o:p></o:p></span></strong></p> <p class=MsoNormal style='mso-margin-top-alt:auto;mso-margin-bottom-alt:auto; text-align:justify'><span style='font-size:16.0pt'><u2:p></u2:p>Research (with Dr I S Blagbrough) is centred around the exploitation of a very potent natural product alkaloid lead compound, methyllycaconitine, the value of which was apparent in Roman times, for the design and synthesis of novel small molecule antagonists at the nicotinic acetylcholine receptor. The project employs a range of synthetic techniques to prepare novel polycycles, which are evaluated for nicotinic antagonist potency in the Department of Biology and Biochemistry (with Professor S J Wonnacott). Potent small molecule mimics have been designed that have potential for use in neurodegenerative diseases and as safer insecticides.</span></p> </td> </tr> <tr style='mso-yfti-irow:3;mso-yfti-lastrow:yes'> <td style='padding:4.5pt 4.5pt 4.5pt 4.5pt'> <div align=center> <table class=MsoNormalTable border=1 cellpadding=0 width="99%" style='width:99.0%;mso-cellspacing:1.5pt;mso-padding-alt:0cm 5.4pt 0cm 5.4pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal>&nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:1'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=216 height=219 id="_x0000_i1683" src=pic10.jpg></h5> </td> </tr> <tr style='mso-yfti-irow:2'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:3'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=219 height=180 id="_x0000_i1684" src=pic11.jpg alt=pic11></h5> </td> </tr> <tr style='mso-yfti-irow:4'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:5'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=219 height=209 id="_x0000_i1685" src=pic6.jpg></h5> </td> </tr> <tr style='mso-yfti-irow:6'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:7'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=219 height=209 id="_x0000_i1686" src=pic7.jpg></h5> </td> </tr> <tr style='mso-yfti-irow:8'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:9'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=219 height=209 id="_x0000_i1687" src=pic8.jpg></h5> </td> </tr> <tr style='mso-yfti-irow:10'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:11'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=219 height=274 id="_x0000_i1688" src=pic9.jpg alt=pic9></h5> </td> </tr> <tr style='mso-yfti-irow:12'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:13'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><o:p>&nbsp;</o:p></p> </td> </tr> <tr style='mso-yfti-irow:14'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:15;mso-yfti-lastrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><!--[if gte vml 1]><v:shape id="iimg_-1619019644" o:spid="_x0000_s1027" type="#_x0000_t75" alt="pic14" style='position:absolute; margin-left:0;margin-top:0;width:164.25pt;height:175.5pt;z-index:1; mso-wrap-distance-left:0;mso-wrap-distance-top:0; mso-wrap-distance-right:0;mso-wrap-distance-bottom:0; mso-position-horizontal:left;mso-position-horizontal-relative:text; mso-position-vertical-relative:line' o:allowoverlap="f"> <v:imagedata src="pic14.jpg"/> <w:wrap type="square"/> </v:shape><![endif]--><![if !vml]><img width=219 height=234 src=pic14.jpg align=left alt=pic14 border=1 v:shapes="iimg_-1619019644"><![endif]></p> </td> </tr> </table> </div> <p class=MsoNormal align=center style='text-align:center'><b><span style='display:none;mso-hide:all'><o:p>&nbsp;</o:p></span></b></p> <div align=center> <table class=MsoNormalTable border=1 cellpadding=0 width="99%" style='width:99.0%;mso-cellspacing:1.5pt;mso-padding-alt:0cm 5.4pt 0cm 5.4pt'> <tr style='mso-yfti-irow:0;mso-yfti-firstrow:yes'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5 style='margin:0cm;margin-bottom:.0001pt'><span style='font-size:14.0pt'><br> <span style='color:red'>Journal covers designed by, or featuring work from, the research group:<br> </span></span><!--[if gte vml 1]><v:shape id="iimg_-1423723579" o:spid="_x0000_s1028" type="#_x0000_t75" alt="Cover9" style='position:absolute;margin-left:0; margin-top:0;width:189.75pt;height:226.15pt;z-index:2; mso-wrap-distance-left:0;mso-wrap-distance-top:0; mso-wrap-distance-right:0;mso-wrap-distance-bottom:0; mso-position-horizontal:left;mso-position-horizontal-relative:text; mso-position-vertical:top;mso-position-vertical-relative:line' o:allowoverlap="f"> <v:imagedata src="file:///H:\public_html\cover9.jpg%3f__scale=t:4,c:FFFFFF,w:219,h:261"/> <w:wrap type="square"/> </v:shape><![endif]--><![if !vml]><img width=253 height=302 src="file:///H:\public_html\cover9.jpg%3f__scale=t:4,c:FFFFFF,w:219,h:261" align=left alt=Cover9 v:shapes="iimg_-1423723579"><![endif]><span style='font-size:14.0pt;color:red'><o:p></o:p></span></h5> </td> </tr> <tr style='mso-yfti-irow:1'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5>&nbsp;<a name=ChemComm></a></h5> </td> </tr> <tr style='mso-yfti-irow:2'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:3'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=254 height=348 id="_x0000_i1689" src="file:///H:\public_html\cover1.jpg%3f__scale=w:219,h:300,t:4,c:FFFFFF" alt="ACS Chemical Biology"></h5> </td> </tr> <tr style='mso-yfti-irow:4'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:5'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=250 height=342 id="_x0000_i1690" src=cover2.jpg alt="Angewandete Chemie"></h5> </td> </tr> <tr style='mso-yfti-irow:6'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><!--[if gte vml 1]><v:shape id="iimg_-606398970" o:spid="_x0000_s1029" type="#_x0000_t75" alt="pic5.jpg" style='position:absolute;margin-left:0; margin-top:0;width:186pt;height:242.9pt;z-index:3; mso-wrap-distance-left:0;mso-wrap-distance-top:0; mso-wrap-distance-right:0;mso-wrap-distance-bottom:0; mso-position-horizontal:left;mso-position-horizontal-relative:text; mso-position-vertical:top;mso-position-vertical-relative:line' o:allowoverlap="f"> <v:imagedata src="file:///H:\public_html\cover3.jpg%3f__scale=w:219,h:286,t:4,c:FFFFFF"/> <w:wrap type="square"/> </v:shape><![endif]--><![if !vml]><img width=248 height=324 src="file:///H:\public_html\cover3.jpg%3f__scale=w:219,h:286,t:4,c:FFFFFF" align=left alt=pic5.jpg v:shapes="iimg_-606398970"><![endif]><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:7'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><o:p>&nbsp;</o:p></p> </td> </tr> <tr style='mso-yfti-irow:8'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> <!--[if gte vml 1]><v:shape id="iimg_-604182354" o:spid="_x0000_s1030" type="#_x0000_t75" alt="ChemComm" style='position:absolute;margin-left:0; margin-top:0;width:183pt;height:239.5pt;z-index:4; mso-wrap-distance-left:3.75pt;mso-wrap-distance-top:3.75pt; mso-wrap-distance-right:3.75pt;mso-wrap-distance-bottom:3.75pt; mso-position-horizontal:left;mso-position-horizontal-relative:text; mso-position-vertical:top;mso-position-vertical-relative:line' o:allowoverlap="f"> <v:imagedata src="file:///H:\public_html\cover4.jpg%3f__scale=w:217,h:284,t:4,c:FFFFFF"/> <w:wrap type="square"/> </v:shape><![endif]--><![if !vml]><img width=244 height=319 src="file:///H:\public_html\cover4.jpg%3f__scale=w:217,h:284,t:4,c:FFFFFF" align=left hspace=5 vspace=5 alt=ChemComm v:shapes="iimg_-604182354"><![endif]>&nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:9'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><o:p>&nbsp;</o:p></p> </td> </tr> <tr style='mso-yfti-irow:10'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:11'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=248 height=354 id="_x0000_i1691" src=cover5.jpg alt="Trends in Pharmaceutical Science"></h5> </td> </tr> <tr style='mso-yfti-irow:12'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:13'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=250 height=336 id="_x0000_i1692" src=cover6.jpg alt="FEBS Letters"></h5> </td> </tr> <tr style='mso-yfti-irow:14'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:15'> <td style='padding:.75pt .75pt .75pt .75pt'> <h5><img border=0 width=250 height=332 id="_x0000_i1693" src=cover7.jpg alt=BBRC></h5> </td> </tr> <tr style='mso-yfti-irow:16'> <td style='padding:.75pt .75pt .75pt .75pt'> <p class=MsoNormal><br> &nbsp;</p> </td> </tr> <tr style='mso-yfti-irow:17;mso-yfti-lastrow:yes;height:87.6pt'> <td style='padding:.75pt .75pt .75pt .75pt;height:87.6pt'> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><span style='font-weight:normal'><!--[if gte vml 1]><v:shape id="_x0000_i1849" type="#_x0000_t75" style='width:184.5pt;height:231pt'> <v:imagedata src="index_files/image008.jpg" o:title="cover12"/> </v:shape><![endif]--><![if !vml]><img border=0 width=246 height=308 src="index_files/image009.jpg" v:shapes="_x0000_i1849"><![endif]><o:p></o:p></span></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><!--[if gte vml 1]><v:shape id="_x0000_s1037" type="#_x0000_t75" style='position:absolute;margin-left:2.55pt;margin-top:8.5pt;width:177pt; height:235.5pt;z-index:5;mso-position-horizontal:absolute; mso-position-vertical:absolute' stroked="t" strokeweight="1.5pt"> <v:imagedata src="index_files/image012.png" o:title=""/> </v:shape><![if gte mso 9]><o:OLEObject Type="Embed" ProgID="AcroExch.Document.7" ShapeID="_x0000_s1037" DrawAspect="Content" ObjectID="_1398859098"> </o:OLEObject> <![endif]><![endif]--><![if !vml]><span style='mso-ignore:vglayout'> <table cellpadding=0 cellspacing=0 align=left> <tr> <td width=1 height=9></td> </tr> <tr> <td></td> <td><img width=240 height=318 src="index_files/image015.jpg" v:shapes="_x0000_s1037"></td> </tr> </table> </span><![endif]><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <br style='mso-ignore:vglayout' clear=ALL> <h5><img border=0 width=245 height=332 id="_x0000_i1842" src=cover11.jpg alt="Chemical Biology"></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> <h5><o:p>&nbsp;</o:p></h5> </td> </tr> </table> </div> <p class=MsoNormal align=center style='text-align:center'><b><o:p></o:p></b></p> </td> <td valign=top style='padding:4.5pt 4.5pt 4.5pt 4.5pt'> <h5 align=center style='text-align:center'><span style='font-size:20.0pt; color:red'>Selected Publications<o:p></o:p></span></h5> <h4>2012</h4> <p class=MsoNormal><span class=MsoLineNumber><span style='font-size:10.0pt; font-family:"Times New Roman"'><a href="ACSEnvirScipublished2012.pdf">Determination<span style='mso-spacerun:yes'>  </span>of <i style='mso-bidi-font-style:normal'>neo</i>- and <span style='font-variant:small-caps'>d</span>-<i style='mso-bidi-font-style: normal'>chiro</i>-inositol hexakisphosphate in soils by solution <sup>31</sup>P NMR spectroscopy</a><o:p></o:p></span></span></p> <p class=MsoNormal style='mso-outline-level:1'><span style='font-size:10.0pt'>B L Turner, A <st1:place w:st="on">W Cheeseman</st1:place>,<span style='mso-spacerun:yes'>  </span>H Y Godage, A M. Riley and <b style='mso-bidi-font-weight:normal'>B V L Potter</b><span style='mso-spacerun:yes'>  </span></span><i style='mso-bidi-font-style:normal'><span lang=EN-US style='font-size:10.0pt;mso-ansi-language:EN-US'>ACS Environmental Sci Tech</span></i><span lang=EN-US style='font-size:10.0pt;mso-ansi-language: EN-US'> (2012) </span><b style='mso-bidi-font-weight:normal'><span style='font-size:10.0pt'>46</span></b><span style='font-size:10.0pt'>, 4994-5002.</span><sup><o:p></o:p></sup></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'><a href="SHIP2%20paper2012published.pdf">A synthetic polyphosphoinositide headgroup surrogate in complex with SHIP2<span style='mso-spacerun:yes'>  </span>reveals options for drug discovery.</a><o:p></o:p></span></p> <p class=MsoPlainText style='text-align:justify'><span lang=EN-US style='font-family:"Times New Roman"'>S J Mills, C Persson, G Cozier, M P Thomas, L Trésaugues, C Erneux, A M Riley, P Nordlund and <b style='mso-bidi-font-weight:normal'>B V L Potter</b><i style='mso-bidi-font-style: normal'> ACS Chem Biol</i> (2012) <b style='mso-bidi-font-weight:normal'>7</b>, 822</span><span lang=EN-US style='font-family:"Times New Roman";mso-fareast-font-family: AdvOT8608a8d1+22'>"</span><span lang=EN-US style='font-family:"Times New Roman"'>828 <o:p></o:p></span></p> <p class=ElsArticleTitle style='margin:0cm;margin-bottom:.0001pt;line-height: normal'><span lang=EN-US style='font-size:12.0pt;mso-bidi-font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=ElsArticleTitle style='margin:0cm;margin-bottom:.0001pt;line-height: normal'><span lang=EN-US style='font-size:10.0pt'>Synthesis and evaluation of A-ring modified analogues of estrone-3-<i>O</i>-sulfamate as potent steroid sulfatase inhibitors. <o:p></o:p></span></p> <p class=ElsArticleTitle style='margin:0cm;margin-bottom:.0001pt;line-height: normal'><span lang=EN-US style='font-size:10.0pt'>L W L Woo, B Leblond, A<span style='mso-spacerun:yes'>  </span>Purohit and <b style='mso-bidi-font-weight: normal'>B V L Potter</b><span style='mso-spacerun:yes'>  </span><i style='mso-bidi-font-style:normal'>Bioorg Med Chem</i> (2012) <b style='mso-bidi-font-weight:normal'><span style='color:#000066'>20</span></b><span style='color:#000066'>, 2506 2519.</span><o:p></o:p></span></p> <p class=MsoNormal><span lang=EN-US style='mso-ansi-language:EN-US; mso-fareast-language:EN-US'><o:p>&nbsp;</o:p></span></p> <p class=BATitle><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"; font-weight:normal'><a href="JMCchristelle2012published.pdf">An Aberrant Cyclization Affords a Cyclic Adenosine 5<span style='font-family:Symbol; mso-ascii-font-family:"Times New Roman";mso-hansi-font-family:"Times New Roman"; mso-char-type:symbol;mso-symbol-font-family:Symbol'><span style='mso-char-type: symbol;mso-symbol-font-family:Symbol'>¢</span></span>-Diphosphoribose Analog Modified at C-6 with Biological Activity in Jurkat T Cells.</a><o:p></o:p></span></p> <p class=BATitle><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"; font-weight:normal'>C Moreau, T Kirchberger, M P Thomas, K Weber, A H<span style='mso-spacerun:yes'>  </span>Guse and<span style='mso-spacerun:yes'>  </span></span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"'>B V L Potter</span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"; font-weight:normal'> <i style='mso-bidi-font-style:normal'>J Med Chem</i> (2012)<span style='mso-spacerun:yes'>  </span></span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"'>55</span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman";font-weight: normal'>, 1478-1489<o:p></o:p></span></p> <p class=BATitle style='line-height:normal'><span lang=EN-US style='font-size:12.0pt;font-family:"Times New Roman";mso-fareast-language: EN-GB;mso-bidi-font-weight:bold;mso-no-proof:no'><o:p>&nbsp;</o:p></span></p> <p class=BATitle style='line-height:normal'><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman";font-weight:normal'><a href="JOCpublished2012.pdf">Total Synthesis of a Cyclic Adenosine 52 -Diphosphate Ribose Receptor Agonist.</a><o:p></o:p></span></p> <p class=BATitle style='line-height:normal'><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman";font-weight:normal'>J M Swarbrick and </span><span lang=EN-US style='font-size:10.0pt;font-family: "Times New Roman"'>B V L Potter</span><span lang=EN-US style='font-size:10.0pt; font-family:"Times New Roman";font-weight:normal'> <i style='mso-bidi-font-style: normal'>J Org Chem</i> (2012)</span><span lang=EN-US> </span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman"'>77</span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman";font-weight: normal'>, 4191-4197</span><span lang=EN-US style='font-size:12.0pt; font-family:"Times New Roman";font-weight:normal'> </span><span lang=EN-US style='font-size:10.0pt;font-family:"Times New Roman";font-weight:normal'><span style='mso-spacerun:yes'> </span><a href="JOCcover2012published.pdf">[Featured Article, <b style='mso-bidi-font-weight:normal'>with journal cover design</b>].</a></span><span lang=EN-US style='font-size:12.0pt;font-family:"Times New Roman";font-weight: normal'><o:p></o:p></span></p> <p class=MsoNormal><span lang=EN-US style='font-size:10.0pt;mso-ansi-language: EN-US;mso-fareast-language:EN-US'><o:p>&nbsp;</o:p></span></p> <p class=MsoPlainText style='text-align:justify'><span lang=EN-US style='font-family:"Times New Roman"'><a href="JMCsureshanpublished.pdf">Contribution of Phosphates and Adenine to the Potency of Adenophostins at the InsP<sub>3</sub> Receptor: Synthesis of all Possible Bisphosphates of Adenophostin A.</a><o:p></o:p></span></p> <p class=MsoPlainText style='text-align:justify'><span lang=EN-US style='font-family:"Times New Roman"'>K M Sureshan, A M Riley, S C Tovey, C W Taylor and <b style='mso-bidi-font-weight:normal'>B V L Potter</b> <i style='mso-bidi-font-style:normal'>J Med Chem</i> (2012) <b style='mso-bidi-font-weight: normal'>55</b>, 1706-1720.<o:p></o:p></span></p> <p class=MsoPlainText style='text-align:justify'><span lang=EN-US style='font-family:"Times New Roman"'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'><a href="ml200232c.pdf">Steroidomimetic tetrahydroisoquinolines for the design of new microtubule disruptors</a><o:p></o:p></span></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'>M P<span style='mso-spacerun:yes'>  </span>Leese, W Dohle, F Jourdan, M Kimberley, R Bai,<sup> </sup>E Hamel, E Ferrandis<sup> </sup>and <b style='mso-bidi-font-weight:normal'>B V L Potter</b> <i style='mso-bidi-font-style: normal'>ACS MedChemLett</i> (2012) <b style='mso-bidi-font-weight:normal'>3</b>, 5-9<o:p></o:p></span></p> <h4>2011</h4> <div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="ChemMedChemSTSpublished.pdf">Structure-Activity Relationship of the Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495)</a>. <o:p></o:p></span></p> <p class=MsoNormal><span style='font-size:10.0pt'>L W L Woo, D Ganeshapillai,M P Thomas,O B Sutcliffe, B&nbsp;Malini, M&nbsp;F&nbsp;<st1:City w:st="on"><st1:place w:st="on">Mahon</st1:place></st1:City>,&nbsp;&nbsp;A&nbsp;Purohit and <strong>B V L Potter</strong> <i>ChemMedChem</i> (2011)</span> <b style='mso-bidi-font-weight:normal'><span style='font-size:10.0pt'>6, </span></b><span style='font-size:10.0pt'>2109-2034</span><b style='mso-bidi-font-weight:normal'> </b><span style='font-size:10.0pt'><span style='mso-spacerun:yes'> </span><o:p></o:p></span></p> </div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="cover12.jpg">[VIP paper with <b style='mso-bidi-font-weight:normal'>journal cover feature</b>]</a><o:p></o:p></span></p> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> <div style='margin-top:5.0pt;margin-bottom:5.0pt'> <p class=MsoNormal><span style='font-size:10.0pt'><a href="CMCadamantylethanone1616_ftp.pdf">Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human cellular 11²-hydroxysteroid dehydrogenase type 1</a>. <br> X Su, F Pradaux-Caggiano, N Vicker, M P Thomas, H Halem, M D Culler and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>ChemMedChem</i> (2011)&nbsp;<b style='mso-bidi-font-weight:normal'>6</b>, 1616-1629.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal><span style='font-size:10.0pt'>Structure-activity relationships of C-17-substituted estratriene-3-O-sulfamates as anticancer agents.<br> F Jourdan, M P Leese, W Dohle, E Ferrandis, S P Newman, S Chander, A Purohit and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>J Med Chem</i> (2011) <b style='mso-bidi-font-weight:normal'>54</b>, 4863-4879.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;&nbsp;<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="CMCAromataseVorozole1423_ftp.pdf">Aromatase and Dual Aromatase-Steroid Sulfatase Inhibitors from the Letrozole and Vorozole Templates</a>.<br> P M Wood, L W Lawrence Woo, M P Thomas, M F Mahon, A Purohit and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>ChemMedChem</i> (2011) <b style='mso-bidi-font-weight:normal'>6</b>, 1423-1438.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="CMCadamantylheterocyclic1439_ftp.pdf">Discovery of adamantyl heterocyclic ketones as potent human cellular 11²-hydroxysteroid dehydrogenase type 1 inhbitors.</a> <br> X Su, N Vicker, M P Thomas, F Pradaux-Caggiano, H Halem, M D Culler and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>ChemMedChem</i> (2011) <b style='mso-bidi-font-weight:normal'>6</b>, 1439-1451.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="OBCcADPRJan2011published.pdf" target="_blank" title="synthesis of cylcic adenosine 5'-diphosphate ribose analogues">Synthesis of cyclic adenosine 5'-diphosphate ribose analogues: a C2' endo/syn  southern ribose conformation underlies activity at the sea urchin cADPR receptor</a>.<br> C Moreau, G A Ashamu, V C Bailey, A Galione, A H Guse and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>Org Biomol Chem </i>(2011) <strong>9</strong>, 278-290.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> </div> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'>Development of Steroid Sulfatase Inhibitors.<o:p></o:p></span></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'>L W L Woo, A Purohit and <b>B V L Potter</b>, <i style='mso-bidi-font-style: normal'>Mol Cell Endocrinol</i> (2011) <b style='mso-bidi-font-weight:normal'>340</b>, 175-185.<o:p></o:p></span></p> <p class=MsoNormal style='text-align:justify'><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> <div> <p class=MsoNormal><span style='font-size:10.0pt'><a href="FMC11betapublished.pdf" target="_self" title="The Crystal Structures of 11²-Hydroxysteroid Dehydrogenase Type 1 and Their Use in Drug Discovery.">The Crystal Structures of 11²-Hydroxysteroid Dehydrogenase Type 1 and Their Use in Drug Discovery.</a><br> MP Thomas &amp; <strong>BVL Potter</strong>, <i style='mso-bidi-font-style: normal'>Future Med Chem</i> (2011)&nbsp;<b style='mso-bidi-font-weight:normal'>3</b>, 367-390.<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>&nbsp;<o:p></o:p></span></p> </div> <div> <p class=MsoNormal><span style='font-size:10.0pt'>Steroid Sulfatase: A Pivotal Player in Estrogen Synthesis and Metabolism.<br> A Purohit, L W L Woo and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style: normal'>Mol Cell Endocrinol</i> (2011) <b style='mso-bidi-font-weight:normal'>340</b>, 154-160.<br> <br> Hybrid Dual Aromatase-Steroid Sulfatase Inhibitors with Exquisite Picomolar Inhibitory Activity.<br> L W L Woo, C A Bubert, A Purohit, and<strong> B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>ACS MedChemLett</i> (2011) <b style='mso-bidi-font-weight:normal'>2</b>, 243-247.<o:p></o:p></span></p> </div> <h4>2010</h4> <p><span style='font-size:10.0pt'><a href="BJPadenophostinformalreprint.pdf" target="_blank" title="Selective Determinants">Selective Determinants of IP<sub>3 </sub>and Adenophostin A Interactions with Type 1 IP<sub>3</sub> Receptors. </a><br> A M Rossi, K M Sureshan, A M Riley, <strong>B V L Potter </strong>&amp; C W Taylor, <i style='mso-bidi-font-style:normal'>Brit J Pharmacol</i> (2010) <b>161, </b>1070 1085.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Bicyclic derivatives of the potent Dual Aromatase-Steroid Sulfatase Inhibitor 2-bromo-4-(((4-cyanophenyl)(4<em>H</em>-1,2,4-triazol-4-yl)amino)methyl)phenyl sulfamate: Synthesis, SAR, Crystal Structure, <em>in vitro</em> and <em>in vivo</em> Activities.<br> P M Wood, L W L Woo, J-R Labrosse, M P Thomas, M F Mahon, S K Chander, A Purohit, M J Reed and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style: normal'>Chem MedChem</i> (2010) <strong>5,</strong> 1577-1593.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="Potter-BRAINjul2010published.pdf" target="_blank" title="NAADP mediated Ca2+ signaling in effector cells">NAADP mediated Ca<sup>2+ </sup>signaling in effector cells regulates autoimmunity of the nervous system. </a><br> C Cordiglieri, F Odoardi, B Zhang, M Nebel, N Kawakami WEF Klinkert, D Lodygin, F Lühder, E Breunig, D Schild, V Kumar Ulaganathan, K Dornmair, <b>B V L Potter</b>, A H Guse and A Flügel, <i style='mso-bidi-font-style:normal'>Brain</i> (2010) <b style='mso-bidi-font-weight:normal'>133</b>, 1930</span><span style='font-size:10.0pt;font-family:Tahoma'> </span><span style='font-size: 10.0pt'>1943.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Discovery of adamantyl ethanone derivatives as potent 11²-hydroxysteroid dehydrogenase type 1 inhibitors.<br> X Su, F Pradaux-Caggiano, M P Thomas, M Szeto, H Halem, M D Culler, N Vicker, and <b>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>ChemMedChem</i> (2010) <b style='mso-bidi-font-weight:normal'>7</b>, 1026-1044.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Structures of four human carbonic anhydrase II/inhibitor complexes reveal a second binding site for steroidal and non-steroidal inhibitors.<br> G Cozier, MP Leese, M D Lloyd, M Baker, N Thiyagarajan, K R Acharya and <b>B V L Potter </b><i style='mso-bidi-font-style:normal'>Biochemistry</i> (2010) <b style='mso-bidi-font-weight:normal'>49</b>,3464-3476.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Binding of IP<sub>3</sub> and Adenophostin A to the N-terminal Region of the IP<sub>3 </sub>Receptor: Thermodynamic Analysis Using Fluorescence Polarization with a Novel IP<sub>3</sub> Receptor Ligand.<br> S Z Ding, A M Rossi, A M Riley, T Rahman, <b>B V L Potter</b> and C W Taylor, <i style='mso-bidi-font-style:normal'>Mol Pharmacol.</i> (2010) <b style='mso-bidi-font-weight:normal'>77</b>, 995-1004.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Chimeric Microtubule Disruptors.<br> M P Leese, F L Jourdan, M R Kimberley, G Cozier, N Thiyagarajan, C Stengel, S Regis-Lydi, P A Foster, S P Newman, K R Acharya, E Ferrandis, A Purohit, M J Reed and <b>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>Chem Comm</i> (2010) <b style='mso-bidi-font-weight:normal'>46</b>, 2907-2909.<br> <a href="http://www.rsc.org/Publishing/Journals/cb/Volume/2010/05/novel_approach.asp" target="_self" title="Highlights in Chemical Biology">Highlights in Chemical Biology April 2010</a><span style='mso-spacerun:yes'>  </span>and<b style='mso-bidi-font-weight:normal'> <a href="cover11.jpg">Cover feature</a></b><br> <a href="Cover9.jpg">ChemComm Cover feature</a><o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Synthesis, Antitubulin and Anti-proliferative SAR of Analogues of 2-Methoxy-estradiol-3,17-O,O-bissulfamates.<br> F Jourdan, M P Leese, W Dohle, E Hamel, E Ferrandis, S P Newman, A Purohit, M J Reed and <b>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>J Med Chem</i> (2010) <b style='mso-bidi-font-weight:normal'>53</b>, 2942-2951.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.<br> L W L Woo, T Jackson, A Putey, G Cozier, P Leonard, K R Acharya, S K Chander, A Purohit, M J Reed and <b>B V L Potter</b>, <i style='mso-bidi-font-style: normal'>J Med Chem</i> (2010) <b style='mso-bidi-font-weight:normal'>53</b>, 2155-2170.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>A novel inhibitor of the PI3K/Akt pathway based on the structure of inositol 1,3,4,5,6 pentakisphosphate.<br> M Falasca, D Chiozzotto, H Y Godage, M Mazzoletti, A M Riley, S Previdi, <b>B V L Potter</b><i>, </i>M Broggini and T Maffucci, <i style='mso-bidi-font-style: normal'>Brit J Cancer<span style='mso-bidi-font-style:italic'> </span></i>(2010) <b style='mso-bidi-font-weight:normal'>102</b>, 104-114.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Class III beta-tubulin expression and <i>in vitro</i> resistance to microtubule targeting agents.<br> C Stengel, S P Newman, M P Leese, <b>B V L Potter</b>, M J Reed and A Purohit, <i style='mso-bidi-font-style:normal'>Brit J Cancer</i> (2010) <b style='mso-bidi-font-weight:normal'>102</b>, 316-324.<o:p></o:p></span></p> <h4>2009</h4> <p><span style='font-size:10.0pt'><a href="JBC2FNAD09published.pdf" target="_blank" title="Structural Basis for Enzymatic Evolution">Structural Basis for Enzymatic Evolution from a Dedicated ADP-ribosyl cyclase to a Multiple Functional NAD Hydrolase.</a><br> Q Liu, R Graeff, I A Kriksunov, H Jiang, B Zhang, N Oppenheimer, H Lin, <b>B V L Potter</b>, H C Lee and Q Hao, <i style='mso-bidi-font-style:normal'>J Biol Chem</i> (2009) <b style='mso-bidi-font-weight:normal'>284</b>(40), 27637-27645.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="JBIC.pdf" target="_blank" title="The behaviour of inositol">The behaviour of inositol 1,3,4,5,6-pentakisphosphate in the presence of the major biological metal cations.</a><br> N Veiga, J Torres, H Y Godage, A M Riley, S Domínguez, <b>B V L Potter</b>, A Díaz and C Kremer, <i style='mso-bidi-font-style:normal'>J Biol Inorg Chem</i> (2009) <b style='mso-bidi-font-weight:normal'>14</b>, 1001-1013.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Determination of the absolute configuration of aromatase and dual aromatase-sulfatase inhibitors by vibrational and electronic circular dichroism spectral analysis.<br> S Abbate, G Longhi, E Castiglioni, F Lebon, P M Wood, L W L Woo and <b>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>Chirality</i> (2009) <b style='mso-bidi-font-weight:normal'>21</b>, 802-808.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="376%20-%20Rossi%20et%20al.pdf">Synthetic partial agonists reveal key steps in IP<sub>3</sub> receptor activation.</a><u><span style='color:blue'><br> </span></u>A M Rossi, A M Riley, S C Tovey, T Rahman, O Dellis,&nbsp;E J A <st1:City w:st="on">Taylor</st1:City>, V G Veresov,&nbsp; <b>B V L Potter</b>&nbsp;and C <st1:place w:st="on">W Taylor</st1:place>,<i style='mso-bidi-font-style: normal'> Nature Chem Biol</i> (2009) <b style='mso-bidi-font-weight:normal'>5</b>(9), 631-639.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="biochemjkirchbergerjul09published.pdf" target="_self" title="8-Bromo-cyclic insone diphosphoribose">8-Bromo-cyclic inosine diphosphoribose: towards a selective cyclic ADP-ribose agonist.</a><br> T Kirchberger, C Moreau, G K Wagner, R Fliegert, C C Siebrands, M Nebel, F Schmid, A Harneit, F Odoardi, A Flügel, <b>B V L Potter </b>and A H Guse, <i style='mso-bidi-font-style:normal'>Biochem J</i> (2009)&nbsp;<b style='mso-bidi-font-weight:normal'>422</b>, 139</span><span style='font-size:10.0pt;font-family:"Courier New"'> </span><span style='font-size:10.0pt'>149.&nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="PNASpublished.pdf" target="_blank">NAADP mediated Ca<sup>2+</sup> signaling via type 1 ryanodine receptor in T cells revealed by a synthetic NAADP antagonist.</a><br> W Dammermann, B Zhang, M Nebel, C Cordiglieri, F Odoardi, T Kirchberger, N Kawakami, J Dowden, F Schmid, K Dornmair, M Hohenegger, A Flügel, A H Guse and <b>B V L Potter</b>,<br> <i style='mso-bidi-font-style:normal'>Proc Natl Acad Sci USA</i> (2009) <b style='mso-bidi-font-weight:normal'>106</b>, 10678-10683.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>The development of steroid sulfatase inhibitors for hormone-dependent cancer therapy.<br> J M Day, A Purohit, H J Tutill, P A Foster, L W L Woo, <b>B V L Potter </b>and M J Reed,&nbsp;<i style='mso-bidi-font-style:normal'>Ann NY Acad Sci</i> (2009) <b style='mso-bidi-font-weight:normal'>1155</b>, 80 87.<br> <br> <a href="chemcommsureshanfeb09published.pdf" target="_blank">Activation of IP<sub>3</sub> receptors by synthetic bisphosphate ligands.</a>&nbsp;<br> K M Sureshan, A M Riley, A M Rossi, S C Tovey,&nbsp;S G Dedos, C W Taylor and <b>B V L Potter,</b> <i style='mso-bidi-font-style:normal'>Chem Comm</i> (2009) 1204-1206.&nbsp;&nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Discovery of Adamantyl Amides as Novel Selective Inhibitors of Human 11²-Hydroxysteroid Dehydrogenase Type 1.<br> X Su, N Vicker, M Trusselle, H Halem, M Culler and <b>B V L Potter</b>,<sup>&nbsp;</sup><i style='mso-bidi-font-style:normal'>Mol Cell Endocrinol</i> (2009) <b style='mso-bidi-font-weight:normal'>301</b>, 169-173.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>The Design of Novel 17²-Hydroxysteroid Dehydrogenase Type 3 Inhibitors.<br> N Vicker, J S Springall, C M Sharland, H V Bailey, A Smith, J M Day, H J Tutill, M J Reed, A Purohit and <b>B V L Potter</b>, <i style='mso-bidi-font-style: normal'>Mol Cell Endocrinol</i> (2009) <b style='mso-bidi-font-weight:normal'>301</b>, 259-265.&nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Development of hormone-dependent prostate cancer models for the evaluation of inhibitors of 17²-hydroxysteroid dehydrogenase Type 3.<br> J M Day, H J Tutill, P A Foster, H V Bailey, W B Heaton, C M Sharland, N Vicker, <b>B V L Potter</b>, A Purohit and M J Reed, <i style='mso-bidi-font-style: normal'>Mol Cell Endocrinol</i> (2009) <b style='mso-bidi-font-weight:normal'>301</b>, 251-258.&nbsp;&nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>BCRP expression does not result in resistance to STX140 in vivo, despite the increased expression of BCRP in A2780 cells in vitro after long-term STX140 exposure.<br> J M Day, P A Foster, H J Tutill, S P Newman, Y T Ho, M P Leese, <b>B V L Potter</b>, M J Reed and A Purohit, <i style='mso-bidi-font-style:normal'>Brit J Cancer</i> (2009) <b style='mso-bidi-font-weight:normal'>100</b>, 476-486.&nbsp;&nbsp;<br> &nbsp;<o:p></o:p></span></p> <h4>2008</h4> <p><span style='font-size:10.0pt'>2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer. S L C Tagg, P A Foster, M P Leese, <b>B V L Potter</b>, M J Reed, A Purohit and S P Newman, Brit J Cancer (2008)&nbsp;99, 1842-1848. &nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Effects of C-17 Heterocyclic substituents on the anticancer activity of 2-ethylestra 1,3,5(10)-triene-3-O-sulfamates: Synthesis, in vitro evaluation and computational modelling.<br> F Jourdan , C Bubert , M P Leese, A Smith , E Ferrandis, S Regis-Lydi, S P Newman, A Purohit, M J Reed and <b>B V L Potter</b>, Org Biomol Chem (2008) 6, 4108-4119.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Synthesis of aromatase inhibitors and dual aromatase-sulfatase inhibitors by linking an arylsulfamate motif to 4-(4H-1,2,4-triazol-4-ylamino)benzonitrile: SAR, crystal structures, in vitro and in vivo activities. <br> C Bubert, L W L Woo, O Sutcliffe, M F Mahon, S K Chander, A Purohit, M J Reed and <strong>B V L Potter</strong>, ChemMedChem (2008) 3, 1708-1730.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>The in vivo properties of STX243: a potent angiogenesis inhibitor.<br> M F C Parsons, P A Foster, S K Chander, R Jhalli, S P Newman, M P Leese, <b>B V L Potter</b>, A Purohit and M J Reed, Brit J Cancer (2008) 99, 1433-1441.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>A new therapeutic strategy against hormone-dependent breast cancer: The preclinical development of a dual aromatase and sulfatase inhibitor.<br> P A Foster, S K Chander, S P Newman, L W L Woo, O B Sutcliffe, C Bubert, D Zhou, S Chen, <b>B V L Potter</b>, M J Reed and A Purohit, Clin Cancer Res (2008) 14(20), 6469-6477.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone dependent endometrial cancer. Steroid sulfatase inhibitors and endometrial cancer.<br> P A Foster, L W L Woo, <strong>B V L Potter</strong>, M J Reed and A Purohit, Endocrinology (2008) 149, 4035-4032.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Efficacy of three potent steroid sulfatase inhibitors: Pre-clinical investigations for their use in the treatment of hormone-dependent breast cancer. <br> P A Foster, S K Chander, M Parsons, S P Newman, R Jhalli, L W L Woo, <strong>B V L Potter</strong>, M J Reed and A Purohit, Breast Cancer Res Treat (2008) 111, 129-138.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>2-MeOE2bisMATE and 2-EtE2bisMATE induce cell cycle arrest and apoptosis in breast cancer xenografts as shown by a novel ex vivo technique.<br> P A Foster, Y T Ho, B Raobaikady, S P Newman, P G Kasprzyk, M P Leese, <strong>B V L Potter</strong>, M J Reed and A Purohit, Breast Cancer Res Treat (2008) 111, 251-260.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Design and synthesis of 4 ,6 -unsaturated cyclic ADP-carbocyclic ribose, a Ca2+-mobilizing agent selectively active in T cells.<br> T Kudoh, T Murayama, M Hashii, H Higashida, T Sakurai, C Maechling, B Spiess, K Weber, A H Guse, M Arisawa, <strong>B V L Potter</strong>, A Matsuda and S Shuto, Tetrahedron (2008) 64, 9754-9765.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Steroid sulphatase inhibitors as a target for the topical treatment of skin disorders.<br> M J Reed, A Purohit, L W L Woo and <strong>B V L Potter</strong> (2008) Drugs Future 33(7), 597-606.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Benzene Polyphosphates as tools for cell signaling: interaction with the PH domain of protein kinase B</span><span style='font-size:10.0pt;font-family:Symbol'>a</span><span style='font-size: 10.0pt'> and inhibition of inositol 1,4,5-trisphosphate 5-phosphatase. <br> S J Mills, F Vandeput, M N Trusselle, S T Safrany, C Erneux and <strong>B V L Potter</strong> ChemBioChem (2008) 9,1757-1766.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Chiral Aromatase and Dual Aromatase-Steroid Sulfatase Inhibitors from the Letrozole Template: Synthesis, Absolute Configuration and In Vitro Activity.<br> P M Wood, L W L Woo, J-R Labrosse, M N Trusselle, S Abbate, G Longhi, E Castiglioni, F Lebon, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2008) 51, 4226-4238.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Anti-cancer steroid sulfatase inhibitors: synthesis, in vitro and in vivo activities, molecular modelling and protein crystallography of a potent fluorinated second-generation agent.<br> L W L Woo, D S Fischer, C M Sharland, M Trusselle, P A Foster, S K Chander, A Purohit, M J Reed, A Di Fiore, G De Simone, C T Supuran and <strong>B V L Potter</strong>, Mol Cancer Ther (2008) 7(8), 2435-2444.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Inhibition of steroid sulphatase activity in endometriotic implants by 667COUMATE: a potential new therapy.<br> A Purohit, L Fusi, J Brosens, D Parish, M S Fernandes, L W L Woo, <strong>B V L Potter</strong> and M J Reed. Human Reproduction (2008) 23, 290-297.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>STX140 is efficacious in vitro and in vivo in taxane resistant breast carcinoma cells.<br> S P Newman, P A Foster, C Stengel, J M Day, Y T Ho, J-G Judde, M Lassalle, G Prevost, M P Leese, <strong>B V L Potter</strong>, M J &nbsp;Reed and A Purohit. Clin Cancer Res (2008) 14(2), 597-606.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Direct Evidence for ArO-S Bond Cleavage upon Inactivation of Pseudomonas aeruginosa Arylsulfatase by Aryl Sulfamates.<br> P Bojarova, E Denehy, I Walker, K Loft, D P De Souza, L W L Woo, <strong>B V L Potter</strong>, M J McConville and S J Williams. ChemBioChem (2008) 9, 613  623.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="Potter_JOC_guanophostin_published.pdf" target="_blank">2-Position Base-Modified Analogs of Adenophostin A as High-Affinity Agonists of the D-myo-Inositol Trisphosphate Receptor: In Vitro Evaluation and Molecular Modeling</a>.<br> K M Sureshan, M Trusselle, S C Tovey, C W Taylor and <strong>B V L Potter</strong>, J Org Chem (2008) 73, 1682-1692. <b>[JOC Featured Article]</b><o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Chemoenzymatic synthesis of 7-deaza cyclic adenosine 5'-diphosphate ribose analogues, membrane permeant modulators of intracellular calcium release.<br> B Zhang, V C Bailey and <strong>B V L Potter</strong>, J Org Chem (2008) 73, 1693-1703.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>17ß-Hydroxysteroid dehydrogenase type 1 and not type 12 is a target for endocrine therapy of hormone-dependent breast cancer.<br> &nbsp;J M Day, S P Newman, Y T Ho, P A Foster, M P Leese, <strong>B V L Potter</strong>, M J Reed and A Purohit, Int J Cancer (2008) 122, 1931-1940.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="Potter_JMC_2deoxycADPR_mar08_published.pdf" target=blank>2'-Deoxy Cyclic Adenosine 5'-Diphosphate Ribose Derivatives: Importance of a 2' Hydroxyl Motif for the Antagonistic Activity of 8-Substituted cADPR Derivatives</a>.<br> B Zhang, G Wagner, K Weber, C Garnham, A Morgan, A Galione, A H Guse and&nbsp;<strong>B V L Potter</strong>, J Med Chem (2008) 51, 1623 1636.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Structure-Activity Relationships of C-17 Cyanated Estratrienes as Anti-cancer agents. <br> M P Leese, F Jourdan, K Gaukroger, M Mahon, S Newman, P Foster, C Stengel, S Regis-Lydi, E Ferrandis, A Di Fiore, G De Simone, C Supuran, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2008) 51, 1295 1308.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1.<br> X Su, N Vicker and <strong>B V L Potter</strong>, Prog Med Chem (2008) 46, 29-130.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Novel Non-steroidal Aromatase Inhibitors Based On a Biphenyl Scaffold: synthesis, in vitro SAR and molecular modelling.<br> T Jackson, L W L Woo, M N Trusselle, A Purohit, M J Reed and <strong>B V L Potter</strong>, Chem Med Chem (2008) 3, 603-618.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Novel Inhibitors of 17ß Hydroxysteroid Dehydrogenase Type 1: Templates for Design.<br> G M Allan, N Vicker, H R Lawrence, H J Tutill, J M Day, M Huchet, E Ferrandis, M J Reed, A Purohit and&nbsp;<strong>B V L Potter</strong>, Bioorg Med Chem (2008) 16, 4438 4456.<o:p></o:p></span></p> <h4>2007</h4> <p><span style='font-size:10.0pt'>The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers.<br> S P Newman, P A Foster, Y T Ho, J M Day, B Raobaikady, P G Kasprzyk, M P Leese, <strong>B V L Potter</strong>, M J Reed and A Purohit. Brit J Cancer (2007) 97, 1673 - 1682.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Dual aromatase-sulfatase inhibitors based on the anastrozole template: synthesis, in vitro SAR, molecular modelling and in vivo activity.<br> T Jackson, L W L Woo, M N Trusselle, S K Chander, A Purohit, M J Reed and<b> B V L Potte</b>r, Org &amp; Biomol Chem (2007) 5, 2940-2952.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Catalysis associated conformational changes revealed by human CD38 complexed with a non-hydrolyzable substrate analog.<br> Q Liu, I A Kriksunov, C Moreau, R Graeff, <b>B V L Potter</b>, H C Lee and Q Hao, J Biol Chem (2007) 282, 24825-24832.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>3,17-Disubstituted 2-alkyestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anti-cancer activity.<br> C Bubert, M P Leese, M F Mahon, E Ferrandis, S Regis-Lydi, P G Kasprzyk, S P Newman, Y T Ho, A Purohit, M J Reed and <b>B V L Potter</b>, J Med Chem (2007) 50, 4431-4443.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Dual aromatase-steroid sulfatase inhibitors.<br> L W L Woo, C Bubert, O B Sutcliffe, A Smith, S K Chander, M F Mahon, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2007) 50, 3540-3560.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'><a href="Mills_-_Chemical_Biology_Paper_-_PUBLISHED.pdf" target="_self">Novel inositol phospholipid headgroup surrogate crystallised in the PH domain of protein kinase <span style='font-family:Symbol'>Ba</span>.</a><br> </span><span lang=DE style='font-size:10.0pt;mso-ansi-language:DE'>S J Mills, D Komander, M N Trusselle, D M F van Aalten and <strong>B</strong> <strong>V L Potter</strong>, ACS Chem Biol (2007) 2 (4), 242-246.&nbsp;<a href="cover1.jpg">Cover feature</a><o:p></o:p></span></p> <p><span lang=DE style='font-size:10.0pt;mso-ansi-language:DE'>Nicotinamide 2-fluoroadenine dinucleotide unmasks the NAD<sup>+</sup> glycohydrolase activity of Aplysia Californica adenosine 5'-diphosphate-ribosyl cyclase.<br> B Zhang, H Muller-Steffner, F Schuber and <strong>B V L Potter</strong>, Biochemistry (2007) 46, 4100-4109.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Biphenyl-2,3 4,5 ,6-pentakisphosphate, a novel inositol polyphosphate surrogate, inhibits the activity of two inositide 5-phosphatases and modulates Ca<sup>2+</sup> responses in rat hepatocytes.<br> F Vandeput, L Combettes, S J Mills, K Backers, A Wohlkonig, J Parys, H De Smedt, L Missiaen, G Dupont, <strong>B V L Potter</strong> and C Erneux, FASEB J (2007) 21, 1481-1491.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Rapid and efficient routes to phosphatidylinositol 3,4,5-trisphosphates via myo-inositol orthobenzoate. <br> K M Sureshan, A M Riley and<b> B V L Potter,</b> Tet Lett (2007) 48 1923-1926.<o:p></o:p></span></p> <h4>2006</h4> <p><span style='font-size:10.0pt'>2-Substituted estradiol bis-sulfamates, multi-targeted anti-tumor agents: Synthesis, in vitro SAR, protein crystallography and in vivo activity.<br> M P Leese, B LeBlond, A Smith, S P Newman, A Di Fiore, G De Simone, C T Supuran, A Purohit, M J Reed and<b> B V L Potter</b>, J Med Chem (2006) 49, 7683-7696.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>3-Hydroxybenzene 1,2,4-trisphosphate, a novel second messenger mimic and unusual substrate for type-I myo-inositol 1,4,5-trisphosphate 5-phosphatase: Synthesis and physicochemistry.<br> S J Mills, H Dozol, F Vandeput, K Backers, T Woodman, C Erneux, B Spiess and <b>B V L Potter</b>, Chem Biochem (2006) 7, 1696-1706.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Cellular effects and metabolic stability of N1-cyclic inosine diphosphoribose and its derivatives.<br> T Kirchberger, G Wagner, J Xu, P Wang, A Gasser, R Fliegert, S Bruhn, F E Lund, L-H Zhang, <b>B V L Potter</b> and A H Guse, Brit J Pharmacol, (2006) 149, 337-344.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>A Systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Synthesis of -C-glucoside trisphosphates based on the conformational restriction strategy.<br> M Terauchi, H Abe, S C Tovey, S G Dedos, C W Taylor, M Paul, M Trusselle and <strong>B V L Potter</strong>, A Matsuda and S Shuto, J Med Chem (2006) 49, 1900-1909.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Design and synthesis of 5'-deoxy-5'-phenyladenophostin A, a highly potent IP3 receptor ligand.<br> T Mochizuki, Y Kondo, H Abe, C W Taylor, <strong>B V L Potter</strong>, A Matsuda and S Shuto, Org Letts (2006) 8 (7), 1455-1458.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Focused libraries of 16 substituted estrone derivatives and modified E-ring steroids: Inhibitors of 17 -hydroxysteroid dehydrogenase type 1.<br> N Vicker, H R Lawrence, G M Allan, C Bubert, A Smith, H J Tutill, A Purohit, J M Day, M F Mahon, M J Reed and <strong>B V L Potter</strong>, Chem Med Chem (2006) 1, 464-481.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Guanophostin A: Synthesis and evaluation of a high affinity agonist of the D-myo-inositol 1,4,5 trisphosphate receptor.<br> K M Sureshan, M Trusselle, S C Tovey, C W Taylor and <strong>B V L Potter</strong>, Chem Comm (2006) 2015-2017.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Regioselective hydrolysis of myo-inositol 1,3,5-orthobenzoate via a 1,2-Bridged 2-phenyl-1',3'-dioxolan-2'-ylium ion provides a rapid route to the anticancer agent Ins(1,3,4,5,6)P5.<br> H Y Godage, A M Riley, T J Woodman and <strong>B V L Potter</strong>, Chem Comm (2006) 2989-2991.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Structural determinants for N1/N7 cyclization of nicotinamide hypoxanthine 5'-dinucleotide (NHD+) derivatives by ADP-ribosyl cyclase from Aplysia Californica: Ca2+-mobilizing activity of 8-substituted cyclic inosine 5'-diphosphoribose analogues in T-lymphocytes.<br> C Moreau, G K Wagner, K Weber, A H Guse and <strong>B V L Potter</strong>, J Med Chem (2006) 49, 5162-5176.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Cell-permeant small-molecule modulators of NAADP-mediated Ca<sup>2+</sup> release.<br> J Dowden, G Berridge, C Moreau, M Yamasaki, G C Churchill, <strong>B V L Potter</strong> and A Galione, Chemistry &amp; Biology (2006) 13, 659-665.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Rapid microwave-assisted reductive amination of ketones with anilines.<br> H V Bailey, W Heaton, N Vicker and <b>B V L Potter</b>, SynLett (2006) 15, 2444-2448.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>scyllo-Inositol pentakisphosphate as an analogue of myo-inositol 1,3,4,5,6-pentakisphosphate: chemical synthesis, physicochemistry and biological applications.<br> A M Riley, M Trusselle, P Kuad, M Borkovec, J Cho, J Choi, X Qian, S B Shears, B Spiess and <strong>B V L Potter</strong>, Chem Bio Chem (2006) 7, 1114-1122.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>In vivo efficacy of STX213, a second generation steroid sulfatase inhibitor for hormone-dependent breast cancer therapy.<br> P A Foster, S P Newman, S K Chander, C Stengel, R Jhalli, L W L Woo, <strong>B V L Potter</strong>, M J Reed and A Purohit, Clin Cancer Res (2006) 12, 5543-5549.<br> <br> Synthesis of Adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP<sub>3 </sub>receptor ligands.<br> T Mochizuki, Y Kondo, H Abe, A Matsuda, S Shuto, S C Tovey, S G Dedos, C W Taylor, M Paul and <strong>B V L Potter</strong>, J Med Chem (2006) 49, 5750-5758.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Phase I study of STX64 (667 Coumate) in breast cancer patients: the first study of a steroid sulphatase inhibitor.<br> S Stanway, A Purohit, L W L Woo, S Sufi, D Vigushin, R Ward, R Wilson, F Z Stanczyk, N Dobbs, E Kulinskaya, M Elliott, <strong>B V L Potter</strong>, M J Reed and&nbsp;R C Coombes Clin Cancer Res (2006) 12 (5) 1585-1592.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>On the contribution of stereochemistry to ITPK1 specificity: Ins(1,4,5,6)P4 is not a physiologic substrate.<br> A M Riley, S Deleu, X Qian, J Mitchell, S-K Chung, S Adelt, G Vogel, <strong>B V L Potter</strong> and S B Shears, FEBS Lett (2006) 324-330.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Chiral desymmetrisation of myo-inositol 1,3,5-orthobenzoate gives rapid access to precursors for second messenger analogues.<br> A M Riley, H Y Godage, M F Mahon and <strong>B V L Potter</strong>, Tetrahedron Asymmetry (2006) 17, 171-174.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Modification of estrone at the 6, 16, 17 positions: Novel potent inhibitors of 17 -hydroxysteroid dehydrogenase type 1.<br> G M Allan, H R Lawrence, J Cornet, D S Fischer, C Bubert, N Vicker, A Smith, H J Tutill, A Purohit, J M Day, M F Mahon, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2006) 49, 1325-1345.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Unusual entry to the novel 8-halo-N1-ribosyl hypoxanthine system by degradation of a cyclic adenosine-5'-diphosphate ribose analogue.<br> C Moreau, T J Woodman and <strong>B V L Potter</strong>, Chem Comm (2006) 1127-1129.<o:p></o:p></span></p> <h4>2005</h4> <p><span style='font-size:10.0pt'>Steroid sulfatase: Molecular biology, regulation and inhibition<br> M J Reed, A Purohit, L W L Woo, S P Newman and <strong>B V L Potter</strong>, Endocrine Reviews (2005) 26 (2), 171-202.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Crystal structure of human carbonic anhydrase II at 1.95 Å resolution in complex with 667-coumate, a novel anti-cancer agent.<br> M D Lloyd, R L Pederick, R Natesh, L W L Woo, A Purohit, M J Reed, K R Acharya and&nbsp;<strong>B V L Potter</strong>, Biochem J (2005) 385, 715-720.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Adenophostin A and analogues modified at the adenine moiety: synthesis, conformational analysis and biological activity.<br> C N Borissow, S J Black, M Paul, S C Tovey, S G Dedos, C W Taylor and <strong>B V L Potter</strong>, Org Biomol Chem (2005) 3, 245-252.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.<br> M D Lloyd, N Thiyagarajan, Y T Ho, L W L Woo, O B Sutcliffe, A Purohit, M J Reed, K R Acharya and <strong>B V L Potter</strong>, Biochemistry (2005) 44, 6858-6866.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Novel and potent 17 -hydroxysteroid dehydrogenase type 1 inhibitors.<br> H R Lawrence, N Vicker, G M Allan, A Smith, M F Mahon, H J Tutill, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2005) 48, 2759-2762.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Rapid synthetic route towards structurally modified derivatives of cyclic adenosine 5'-diphosphate ribose.<br> G K Wagner, A H Guse and <strong>B V L Potter</strong>, J Org Chem (2005) 70, 4810-4819.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Synthesis of stable and cell-type selective analogues of cyclic ADP-ribose, a Ca2+-mobilizing second messenger. Structure-activity relationship of the N1-ribose moiety.<br> T Kudoh, M Fukuoka, S Ichikawa, T Murayama, Y Ogawa, M Hashii, H Higashida, S Kunerth, K Weber, A H Guse, <strong>B V L Potter</strong>, A Matsuda and S Shuto, J Amer Chem Soc (2005) 127, 8846-8855.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Interaction of the catalytic domain of Inositol 1,4,5-trisphosphate 3-kinase A with inositol phosphate analogues.<br> A Poinas, K Backers, A M Riley, S J Mills, C Moreau, <strong>B V L Potter</strong> and C Erneux, Chem Biochem (2005) 6, 1449-1457.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>A-ring substituted estrogen-3-O-sulfamates: Potent multi-targeted anti-cancer agents.<br> M P Leese, H A M Hejaz, M F Mahon, S P Newman, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2005) 48, 5243-5256.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>E-Ring modified steroids as novel potent inhibitors of 17 -hydroxysteroid dehydrogenase type 1.<br> D S Fischer, G M Allan, C Bubert, N Vicker, A Smith, H J Tutill, A Purohit, L Wood, G Packham, M F Mahon, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2005) 48, 5749-5770.pp&nbsp;<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Inhibition of the Phosphatidylinositol 3-kinase/Akt pathway by inositol pentakisphosphate results in antiangiogenic and antitumour effects.<br> </span><span lang=IT style='font-size:10.0pt;mso-ansi-language:IT'>T Maffucci, E Piccolo, A Cumashi, M Iezzi, A M Riley, A Saiardi, H Y Godage, C Rossi, M Broggini, S Iacobelli, <strong>B V L Potter</strong>, P Innocenti and M Falasca, Cancer Research (2005) 65, 8339-8349.<o:p></o:p></span></p> <h4>2004</h4> <p><span style='font-size:10.0pt'>Inhibition of in vitro angiogenesis by 2-methoxy- and 2-ethyl-estrogen sulfamates.<br> S P Newman, M P Leese, A Purohit, D R C James, C E Rennie, <strong>B V L Potter</strong> and M J Reed, Int J Cancer (2004) 109, 533-540.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor or carbonic anhydrases and steroid sulfatase.<br> F Abbate, J-Y Winum, <strong>B V L Potter</strong>, A Casini, J-L Montero, A Scozzafava and C T Supuran, Bioorg Med Chem Lett (2004) 14, 231-234.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Inositol pentakisphosphate promotes apoptosis through the PI 3-K/Akt pathway.<br> </span><span lang=IT style='font-size:10.0pt;mso-ansi-language:IT'>E Piccolo, S Vignati, T Maffucci, P F Innominato, A M Riley, <strong>B V L Potter</strong>, P P Pandolfi, M Broggini, S Iacobelli, P Innocenti and M Falasca, Oncogene (2004) 23, 1754-1765.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Dimers of D-myo-inositol 1,4,5-trisphosphate: Design, synthesis and interaction with Ins(1,4,5)P3 receptors.<br> A M Riley, A J Laude, C W Taylor and <strong>B V L Potter</strong>, Bioconjugate Chem (2004) 15, 278-289.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>2-O-(2-Aminoethyl)-myo-inositol 1,4,5-trisphosphate as a novel ligand for conjugation: physicochemical properties and synthesis of a new Ins(1,4,5)P3 affinity matrix.<br> A M Riley, H Dozol, B Spiess and <strong>B V L Potter</strong>, Biochem Biophys Res Comm (2004) 318, 444-452.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.<br> M P Leese, S P Newman, A Purohit, M J Reed and <strong>B V L Potter</strong>, Bioorg Med Chem Lett (2004) 14, 3135-3138.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>2-MeOE2bisMATE induces caspase-dependent apoptosis in CAL51 breast cancer cells and overcomes resistance to TRAIL via cooperative activation of caspases.<br> L Wood, M P Leese, A Mouzakiti, A Purohit, <strong>B V L Potter</strong>, M J Reed and G Packham, Apoptosis (2004) 9, 323-332.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Amplification and propagation of pacemaker Ca2+ signals by cyclic ADP-ribose and the type 3 ryanodine receptor in T cells.<br> S Kunerth, M F Langhorst, N Schwarzmann, X Gu, L Huang, Z Yang, L Zhang, S J Mills, L-H Zhang, <strong>B V L Potter</strong> and A H Guse, J Cell Sci (2004) 117, 2141-2149.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Inositol trisphosphate analogues selective for types I and II inositol trisphosphate receptors exert differential effects on vasopressin-stimulated Ca2+ inflow and Ca2+ release from intracellular stores in rat hepatocytes.<br> R B Gregory, R Hughes, A M Riley, <strong>B V L Potter</strong>, R A Wilcox and G J Barritt, Biochem J (2004) 381, 519-526.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Novel 18 -Glycyrrhetinic acid analogues as potent and selective inhibitors of 11 -hydroxysteroid dehydrogenases.<br> X Su, H Lawrence, D Gaheshapillai, A Cruttenden, A Purohit, M J Reed, N Vicker and <strong>B V L Potter</strong>, Bioorg Med Chem (2004) 12, 4439-4457.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Chemical synthesis of the second messenger nicotinic acid adenine dinucleotide phosphate by total synthesis of nicotinamide adenine dinucleotide phoshate.<br> J Dowden, C Moreau, R S Brown, G Berridge, A Galione and <strong>B V L Potter</strong>, Angewandte Chemie Int Edn (2004) 43, 4637-4640.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Regulation of casein kinase-2 (CK2) activity by inositol phosphates.<br> L Solyakov, K Cain, B M Tracey, R Jukes, A M Riley, <b>B V L Potter</b>, A B Tobin, J Biol Chem (2004) 279, 43403-43410.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>D-6-Deoxy myo-inositol 1,3,4,5-tetrakisphosphate, a mimic of D-myo-inositol 1,3,4,5-tetrakisphosphate: biological activity and pH-dependent conformational properties.<br> G Horne, C Maechling, A Fleig, M Hirata, R Penner, B Spiess and <strong>B V L Potter</strong>, Biochem Biophys Res Comm (2004) 320, 1262-1270.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Aplysia californica mediated cyclisation of novel 3'-modified NAD analogues: A role for hydrogen bonding in the recognition of cyclic adenosine 5'-diphosphate ribose.<br> C J W Mort, M E Migaud, A Galione and <strong>B V L Potter</strong>, Bioorg Med Chem, (2004) 12, 475-487.<o:p></o:p></span></p> <h4>2003</h4> <p><span style='font-size:10.0pt'>Synthesis and Ca<sup>2+</sup> mobilising activity of purine-modified mimics of adenophostin A: A model for the adenophostin-Ins(1,4,5)P3 receptor interaction.<br> H J Rosenberg, A M Riley, A J Laude, C W Taylor and <strong>B V L Potter</strong>, J Med Chem (2003) 46, 4860-4871.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Identification of mammalian Vps24p as an effector of phosphatidylinositol 3,5 bisphosphate-dependent endosome compartmentalization.<br> P Whitley, B J Reaves, M Hashimoto, A M Riley, <strong>B V L Potter</strong> and G D Holman, J Biol Chem (2003) 278, 38786-38795.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Convergent synthesis and unexpected Ca<sup>2+</sup>-mobilizing activity of the 8-substituted analogues of cyclic ADP-carbocyclic ribose, a stable mimic of Ca<sup>2+</sup>-mobilizing second messenger cyclic ADP-ribose.<br> S Shuto, M Fukuoka, T Kudoh, C Garnham, A Galione, <strong>B V L Potter</strong> and A Matsuda, J Med Chem (2003) 46, 4741-4749.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>First enzymatic synthesis of an N1-cyclised cADPR (cyclic-ADP ribose) analogue with an hypoxanthine partial structure: discovery of a membrane permeant cADPR agonist.<br> G K Wagner, S Black, A H Guse and <strong>B V L Potter</strong>, Chem Comm (2003) 1944-1945.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>First dual aromatase-steroid sulfatase inhibitor.<br> L W L Woo, C Bubert, O B Sutcliffe, A Grasso, S Chander, A Purohit, M J Reed and <strong>B V L Potter</strong>, J Med Chem (2003) 46, 3193-3196.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>D-ring modified estrone derivatives as novel potent inhibitors of steroid sulfatase.<br> D S Fischer, L W L Woo, M F Mahon, A Puroit, M J Reed and <strong>B V L Potter</strong>, Bioorg Med Chem (2003) 11, 1685-1700.<o:p></o:p></span></p> <h4>2002</h4> <p><span style='font-size:10.0pt'>Estrone 3-sulfate mimics, inhibitors of estrone sulfatase activity: Homology model construction and docking studies<br> N M Howarth, A Purohit, J J Robinson, N Vicker, M J Reed and <strong>B V L Potter</strong>, Biochemistry (2002) 41, 14801-14814.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Interactions of inositol 1,4,5-trisphosphate receptors with synthetic poly(ethylene glycol)-linked dimmers of IP<sub>3</sub> suggest close spacing of the IP<sub>3</sub>-binding sites.<br> A M Riley, S A Morris, E P Nerou, V Correa, <strong>B V L Potter</strong> and C W Taylor, J Biol Chem (2002) 277, 40290-40295.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Novel hydrolysis-resistant analogues of cyclic ADP-ribose: Modification of the &quot;northern&quot; ribose and calcium release activity.<br> A H Guse, C Cakir-Kiefer, M Fukuoka, S Shuto, K Weber, V C Bailey, A Matsuda, G W Mayr, N Oppenheimer, F Schuber and <strong>B V L Potter</strong>, Biochemistry (2002) 41, 6744-6751.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Regulation of Ins(3,4,5,6)P<sub>4</sub> signaling by a reversible kinase/phosphatase.<br> M W Y Ho, X Yang, M A Carew, T Zhang, L Hua, Y-U Kwon, S-K Chung, S Adelt, G Vogel, A M Riley, <strong>B V L Potter</strong> and S B Shears, Current Biology (2002) 12, 477-482.<o:p></o:p></span></p> <h4>2001</h4> <p><span style='font-size:10.0pt'>Total synthesis of nucleobase-modified adenophostin A mimics.<br> S Shuto, G Horne, R D Marwood and <strong>B V L Potter</strong>, Chemistry - A European Journal, (2001) 7, 4937-4946.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Bicyclic analogs of D-myo-inositol 1,4,5-trisphosphate related to adenophostin A: Synthesis and biological activity.<br> A M Riley, V Correa, M F Mahon, C W Taylor and <b>B V L Potter</b>, J Med Chem, (2001) 44, 2108-2117.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Structural determinants of adenophostin A activity at inositol trisphosphate receptors.<br> V Correa, A M Riley, S Shuto, G Horne, E P Nerou, R D Marwood, <strong>B V L Potter</strong> and C W Taylor, Mol Pharmacol (2001) 59, 1206-1215.<o:p></o:p></span></p> <h4>2000</h4> <p><span style='font-size:10.0pt'>Nicotinic acid adenine dinucleotide phosphate (NAADP<sup>+</sup>) is an essential regulator of T-lymphocyte Ca<sup>2+</sup>-signaling.<br> I Berg, <strong>B V L Potter</strong>, G W Mayr and A H Guse, J Cell Biol (2000) 150, 581-588.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Synthesis of potent agonists of the D-myo-inositol 1,4,5-trisphosphate receptor based on clustered disaccharide polyphosphate analogues of adenophostin A.<br> M de Kort, V Correa, A R P M Valentijn, G A van der Marel, <strong>B V L Potter</strong>, C W Taylor and J H van Boom, J Med Chem (2000) 43, 3295-3303.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>InsP<sub>4 </sub>facilitates store-operated calcium influx by inhibition of InsP<sub>3</sub> 5-phosphatase.<br> M C Hermosura, H Takeuchi, A Fleig, A M Riley, <strong>B V L Potter</strong>, M Hirata and R Penner, Nature (2000) 408, 735-740.<o:p></o:p></span></p> <h4>1999</h4> <p><span style='font-size:10.0pt'>Structure of the PH domain from Bruton's tyrosine kinase in complex with inositol 1,3,4,5-tetrakisphosphate.<br> E Baraldi, K D Carugo, M Hyvönen, P L Surdo, A M Riley, <strong>B V L Potter</strong>, R O'Brien, J E Ladbury and M Saraste, Structure (1999) 7, 449-460.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Regulation of calcium signalling in T lymphocytes by the second messenger cyclic ADP-ribose.<br> A H Guse, C P da Silva, I Berg, A L Skapenko, K Weber, P Heyer, M Hohenegger, G A Ashamu, H Schulz-Koops, <strong>B V L Potter</strong> and G W Mayr, Nature (1999) 398, 70-73.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Evidence of a role for cyclic ADP-ribose in long-term synaptic depression in hippocampus.<br> M Reyes-Harde, R Empson, <strong>B V L Potter</strong>, A Galione and P K Stanton, Proc Natl Acad Sci USA (1999) 96, 4061-4066.<o:p></o:p></span></p> <h4>1998</h4> <p><span style='font-size:10.0pt'>Steroidal and non-steroidal sulfamates as potent inhibitors of steroid sulfatase.<br> L W L Woo, N M Howarth, A Purohit, H A M Hejaz, M J Reed and <strong>B V L Potter</strong>, J Med Chem (1998) 41, 1068-1083.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>A conformationally restricted cyclic phosphate analogue of inositol trisphosphate: synthesis and physicochemical properties<br> A M Riley, P Guédat, G Schlewer, B Spiess and <strong>B V L Potter</strong>, J Org Chem (1998) 63, 295-305.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Total synthesis from D-xylose of chiral, ring-contracted 1D-myo-inositol 1,4,5-trisphosphate and 1,3,4,5-tetrakisphosphate analogues with C-2 excised.<br> D J Jenkins and <strong>B V L Potter</strong>, J Chem Soc Perkin Trans I (1998) 41-49.<o:p></o:p></span></p> <h4>1997</h4> <p><span style='font-size:10.0pt'>Disaccharide polyphosphates based upon adenophostin A activate hepatic d-myo-inositol 1,4,5-trisphosphate receptors.<br> J S Marchant, M D Beecroft, A M Riley, D J Jenkins, R D Marwood, C W Taylor and <strong>B V L Potter</strong>, Biochemistry (1997) 36, 12780-12790.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Structural analogues of D-myo- inositol 1,4,5-trisphosphate and adenophostin A: Recognition by cerebellar and platelet inositol 1,4,5-trisphosphate receptors.<br> C T Murphy, A M Riley, C J Lindley, D J Jenkins, J Westwick and <strong>B V L Potter</strong>, Mol Pharmacol (1997) 52, 741-748.<o:p></o:p></span></p> <p><span style='font-size:10.0pt'>Rapid synthesis of the enantiomers of myo-inositol 1,3,4,5-tetrakisphosphate by direct chiral desymmetrization of myo-inositol orthoformate.<br> A M Riley, M F Mahon and <strong>B V L Potter</strong>, Angew Chem Int Edn Eng (1997) 36, 1472-1474.<o:p></o:p></span></p> <h4>1996</h4> <p><span style='font-size:10.0pt'>Isotopic enrichment by asymmetric deuteriation. An investigation of the synthesis of deuteriated (S)-(-)-methylsuccinic acids from itaconic acid.<br> D J Hardick, I S Blagbrough and <strong>B V L Potter</strong>, <i style='mso-bidi-font-style:normal'>J Am Chem Soc</i> (1996) 118, 5897-5903.&nbsp;&nbsp;&nbsp;<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>Cyclic aristeromycin diphosphate ribose:<span style='mso-spacerun:yes'>  </span>A potent and poorly hydrolysable Ca<span style='position:relative;top:-3.0pt;mso-text-raise:3.0pt'>2+</span>-mobilising mimic of cyclic adenosine diphosphate ribose.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>V C Bailey, S M Fortt, R J Summerhill, A Galione and <b style='mso-bidi-font-weight:normal'>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>FEBS Lett</i> (1996) <b style='mso-bidi-font-weight:normal'>379</b>, 227-230.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><span style='mso-tab-count:1'>                </span><o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>Active site-directed inhibition of estrone sulfatase by non-steroidal coumarin sulfamates.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>L W L Woo, A Purohit, M J Reed and <b style='mso-bidi-font-weight:normal'>B V L Potter</b>, <i style='mso-bidi-font-style: normal'>J Med Chem</i> (1996) <b style='mso-bidi-font-weight:normal'>39</b>, 1349-1351.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>Synthesis of D-2-deoxy-<i style='mso-bidi-font-style:normal'>myo</i>-inositol 1,3,4,5-tetrakisphosphate from D-glucose.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>D J Jenkins, D Dubreuil and <b style='mso-bidi-font-weight:normal'>B V L Potter,</b> <i style='mso-bidi-font-style: normal'>J Chem Soc Perkin Trans I</i> (1996) 1365-1372.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>A Tandem Horner-Emmons olefination-conjugate addition approach to the synthesis of 1,5-disubstituted-6-azabicyclo[3.2.1]octanes based on the AE ring structure of the norditerpenoid alkaloid methyllycaconitine.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>D J Callis, N F Thomas, D P J Pearson and <b style='mso-bidi-font-weight:normal'>B V L Potter</b>, <i style='mso-bidi-font-style:normal'>J Org Chem</i> (1996) <b style='mso-bidi-font-weight: normal'>61</b>, 4634-4640.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><span style='mso-tab-count:1'>                </span><o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>A specific cyclic ADP-ribose antagonist inhibits cardiac excitation-contraction coupling.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>S Rakovic, A Galione, G A Ashamu, <b style='mso-bidi-font-weight:normal'>B V L Potter</b> and D A Terrar, <i style='mso-bidi-font-style:normal'>Curr Biol</i>, (1996) <b style='mso-bidi-font-weight: normal'>6</b>, 989-996.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>Chiral cyclopentane-based mimics of D-<i style='mso-bidi-font-style:normal'>myo</i>-inositol-1,4,5-trisphosphate from<span style='mso-spacerun:yes'>   </span>D-glucose.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'>D J Jenkins, A M Riley and <b style='mso-bidi-font-weight:normal'>B V L Potter</b>, J Org Chem (1996) <b style='mso-bidi-font-weight:normal'>61</b>, 7719-7726.<o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><span style='mso-tab-count:1'>                </span><o:p></o:p></span></p> <p class=MsoNormal style='margin-left:36.0pt;text-align:justify;text-indent: -36.0pt'><span style='font-size:10.0pt'><o:p>&nbsp;</o:p></span></p> </td> </tr> </table> </div> <p>&nbsp;</p> </div> </body> </html>