Biosketch  

Professor Potter studied chemistry as an Open Exhibitioner at Oxford University, 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 [¹⁶O,¹⁷O,¹⁸O] 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 & Pharmacology, as Head of the Medicinal Chemistry Section.

Fields of research activity are at the interface between Chemistry & Biology and Chemistry & Medicine ie Medicinal & Biological Chemistry, Chemical Biology, Mechanistic Enzymology, Signal Transduction Chemistry, Anticancer Drug Design & Discovery and Translational & Molecular Medicine. [See Cover Gallery]  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 myo-inositol 1,4,5-trisphosphate (IP₃) and the nucleotides cyclic ADP ribose (cADPR) and nicotinic acid adenine dinucleotide phosphate (NAADP). The research group is highly international [See Group Photo Gallery]  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 target steroid sulfatase and in women’s health. Non-steroidal cancer drugs designed at Bath are currently in Phase II clinical trials in metastatic breast cancer, endometrial cancer & prostate cancer  and the steroid derivative PGL2001 is currently in Phase II trials for endometriosis.

 He co-founded the university spin out company Sterix Ltd 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 500 research articles [see eg http://www.researcherid.com/rid/A-1845-2012]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 Lister Institute of Preventive Medicine in 1995. He served on the BBSRC Intracellular Signalling Programme Committee (1992–1996) and the EPSRC Synthetic and Biological Chemistry College (1995–1997) and is a member of the Wellcome Trust Peer Review College (2012-2015). He is a member of the Biochemical Society, the American Association for Cancer Research and the American Chemical Society and was a committee member of the Society for Medicines Research (2002-2006). He was a member of the HEFCE Pharmacy/ Pharmacology Panel for the RAE2001 and RAE2008 exercises and the Research Excellence Framework (REF) Expert Group Panel 2009 and was a member of the Molecules, Genes & Cells Funding Panel of the Wellcome Trust (2006-2011). He is on the editorial boards of the ACS Journal of Medicinal Chemistry (2009-2015), AACR Molecular Cancer Therapeutics (2009-2015), Messenger (2012-) and Future Medicinal Chemistry (2008-), and is a member of the International Advisory Board of ChemMedChem (2014-2017). He has served on the boards of the Biochemical Journal, Carbohydrate Research, Current Organic Synthesis, Drug Design & Discovery and is currently Associate Editor of the Journal of Steroid Biochemistry & Molecular Biology (2009-15) and Editor of the Biochemical Journal's BJChemBio (2009-2016). He received a DSc from Oxford in 1993 and is Visiting Professor of Medicinal Chemistry at Oxford University. He was named in the “H-index ranking of living chemists” listing (current h-index 58).

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 & Medal for Cancer Medicinal Chemistry for 2007/8 with an RSC Endowed Lectureship, the Royal Society of Chemistry Biological & Medicinal Chemistry Sector’s Malcolm Campbell Memorial Prize & Medal for 2009, the GlaxoSmithKline International Achievement Award for 2009 and the Royal Society of Chemistry Interdisciplinary Prize & Medal for 2010 with an RSC Endowed Lectureship. He won the category “Investigator of the Year” at the 2012 European Life Science Awards. He was awarded the RSC-BCMS Endowed Lectureship in Medicinal Chemistry for 2015/16. He was elected to Fellowship of the Academy of Medical Sciences in 2008 and in 2009 to Membership of the Academia Europaea.

X-ray crystal structures of synthetic ligands from the group determined in complex with their target proteins:

Research Interests

Research is centred around four main areas of Chemical Biology and Synthetic Medicinal and Biological Chemistry:

  All projects concern the design, synthesis and biological evaluation of active organic molecules at the interfaces of Chemistry & Biology, ultimately aimed at the dissection of biological mechanisms through chemical biological intervention and molecular biology, or at the interface of Chemistry & Medicine through intelligent drug design & 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 intracellular Ca²⁺. Work is underpinned by in house expression and purification of relevant proteins, biochemical assays, protein crystallography and by in silico 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:

Cyclic ADP-ribose - a new second messenger:

The cyclic nucleotide cyclic adenosine 5'-diphosphate ribose, formed via enzyme-mediated cyclisation of NAD⁺ is a recently identified Ca²⁺-releasing second messenger, that works independently of inositol 1,4,5-trisphosphate. A combination of techniques from total synthesis to chemo-enzymatic methods is  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 University of Hamburg and Oxford University. Recent work has defined SAR parameters for an invertebrate cADPR receptor and also focused upon a total synthesis of a stable active macrocyclic template. [see cover design] Selected ligands are co-crystallised with suitable binding proteins 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 Aplysia californica ADP-ribosyl cyclase with 2-fluoro-NAD⁺. Recent work demonstrates the continuing unusual effects of targeted chemical modification in an active but stable template that we have pioneered, including replacement of the pyrophosphate moiety with retention of biological activity. The use of our stable cIDPR template facilitates structure-based design using ligands co-crystallised with CD38 ectoenzyme for improvement of activity.                           

ADP-ribose, a new second messenger & TRPM2:

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 Hamburg University, to interfere with the ADPR-TRPM2 interaction, that will elucidate structure-activity relationships and may be of potential therapeutic application. The first structure-activity relationship for the TRPM2 ion channel has recently been developed, with nucleotide agonists and antagonists designed

This project is supported by a Wellcome Trust Project Grant.

NAADP - a new second messenger:

The NAD⁺ derivative, nicotinic acid adenine dinucleotide phosphate (NAADP) is a Ca²⁺-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.

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 Hamburg and Oxford. 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 potential in the therapy of autoimmune diseases such as multiple sclerosis and the first small molecules can be designed to illuminate such potential.                                                                           

Anticancer drug design, discovery & translational medicine:

Steroid Sulfatase Inhibitors:
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 17β-estradiol-dependent and hydrolysis of the conjugate estrone 3-O-sulfate by STS is a source of tumour estrogen, especially in situ. 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. Recent work has consolidated the SAR 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) in erythrocytes and transit the liver without undergoing first-pass inactivation. They 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  sulfamate drug : CAII complexes at Bath.

The STS inhibitor PGL2001, designed at Bath,  has the potential to be the first of a new class of drug for benign gynaecological conditions and has entered Phase II clinical trial against endometriosis since 2012. Our non-steroidal drug STX64 [6-oxo-6,7,8,9,10,11-hexahydrocyclo-hepta[c] [1]benzopyran-3-yl sulfamate], formally named Irosustat, a potent tricylic sulfamate derivative, was selected by CRUK for a “first-in-class” clinical trial of a STS inhibitor in women with advanced breast cancer and showed evidence of stable disease. Phase II trials in patients are now complete in endometrial and breast cancer, and further US 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. Irosustat is currently in two breast cancer clinical trials, supported by CRUK.

                                             STX64 - Irosustat

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 picomolar-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.  We proposed the concept of a dual aromatase-sulfatase inhibitor (DASI) 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 IC₅₀s of eg 130pM and 18pM. The movie below shows examples of typical very potent DASIs and the docking of a highly potent biphenyl-based dual inhibitor, designed at Bath, into the active site of human CAII, based upon our X-ray crystal structure of the inhibitor-CAII complex.

     pM active DASIs                

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. 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. The pharmacophoric elements of STX140 are being translated into highly potent chimeric non-steroidal microtubule disruptors with very attractive pharmaceutical properties and activities and this template has considerable potential more widely as a steroidomimetic template that is being actively pursued, for example in a recent dihydroisoquinoline series.

       STX140 & STX140:CAII complex   

Dehydrogenase Inhibition: 17β-Hydroxysteroid dehydrogenases types 1&3(17β-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 both 17β-HSD types 1 & 3 have successfully been demonstrated to exhibit in vivo activity in tumour models.

                 Potent 17β –HSD1 inhibitor

          Potent 17β –HSD3 inhibitor       Docked in homology model

 Efforts directed at novel approaches to diabetes and metabolic syndrome are being pursued by inhibition of the target enzyme 11β-hydroxysteroid dehydrogenase. Low nanomolar active inhibitors have been designed, synthesized and evaluated in whole cell assays using human 11β-HSD transfected HEK293 cells and by protein crystallography. Typical potent examples are shown below:

Research in these areas has been supported by CRUK and through industry.

Novel antagonists at the nicotinic acetylcholine receptor:

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.

                                                                                           Methyllycaconitine

                                                     Selected Publications

2014

In vivo and in vitro properties of STX2484: a non-steroidal anticancer compound active in taxane-resistant cells

C Stengel, S P Newman, S K Chander, F L Jourdan M P Leese, E Ferrandis, S Regis-Lydi, B V L  Potter, M J Reed, A Purohit, and P A Foster Brit J Cancer (2014) 111, 300-308.

Optimisation of  Tetrahydroisoquinoline based Chimeric Microtubule Disruptors

W Dohle, F L Jourdan, C J Chapman, M P Leese, E Hamel,  E Ferrandis and B V L Potter ChemMedChem  (2014) 9, 1783 – 1793.

Synthetic inositol phosphate analogs reveal that PPIP5K2 has a surface-mounted substrate capture site that is a target for drug discovery

H Wang, H Y Godage, A M Riley, J D Weaver, S B Shears  and B V L Potter Chemistry & Biology  (2014) 21, 689–699.

Cellular Internalisation of an Inositol Phosphate Visualised using Fluorescent InsP₅

A M Riley, S Windhorst, Hong-Yin Lin and B V L Potter ChemBioChem (2014) 15, 57–67.

Tetrahydroisoquinoline based steroid-mimetic and chimeric microtubule disruptors

M P  Leese, F Jourdan, M R Major, W Dohle, R Bai, E Hamel, Eric Ferrandis, A Fiore P Kaspryzk, and B V L Potter ChemMedChem (2014) 9, 85-108. [VIP Article with front cover design].

The Enzymes of Human Diphospho-inositol Polyphosphate Metabolism

M P Thomas and B V L Potter FEBS J  (2014) 281, 14-33.

“Click cyclic ADP-ribose”: a neutral second messenger mimic

J M Swarbrick, R Graeff, C Garnham, M P Thomas, A Galione and B V L Potter Chem Comm (2014) 50, 2458-2461.

Synthesis, antitubulin and anti-proliferative SAR of C3/C1 substituted N-benzyl-7-methoxy-6-O-sulfamoyl-1,2,3,4-tetrahydroisoquinolines

W Dohle, M P Leese, F Jourdan, M R Major, R Bai, E Hamel, Eric Ferrandis, A Fiore,  S P Newman, A Purohit  and B V L Potter ChemMedChem (2014)  9, 350 – 370.

Human Genome-Wide RNAi Screen Identifies an Essential Role for Inositol Pyrophosphates in Type-I Interferon Response

N Kudukkil Pulloor, S Nair, A D Kostic, P Bist, J D Weaver, A M Riley, R Tyagi, P D Uchil, John D York, S H Snyder, A García-Sastre, B V L Potter, R Lin, S B Shears, R J Xavier and M N Krishnan PLOS Pathog (2014) 10, e1003981, 1-16.

Synthesis, Anti-proliferative SAR and Antitubulin activity of Steroidomimetic Dihydroisoquinolinones

M P Leese F Jourdan, M R Major, W Dohle, MP Thomas, E Hamel, E Ferrandis, M Mahon, S P Newman, A Purohit and B V L Potter ChemMedChem (2014) 9, 798 – 812  [VIP Article].

2013

Structure-activity relationship of adenosine diphosphoribose at the TRPM2 channel: Rational design of ADPR antagonists

C Moreau, T Kirchberger, JM Swarbrick, S J Bartlett, Y Timur, R Fliegert, T Yorgan A Bauche, A  Harneit, A H Guse and B V L Potter J Med Chem (2013) 56, 10079-102.

CD38 Structure-Based Inhibitor Design using the N1-Cyclic Inosine 5¢-Diphosphate Ribose Template

C Moreau, Q Liu, R Graeff, G K Wagner, J Swarbrick, M P Thomas, S Shuto, H-C. Lee, Q Hao, and B V L Potter PLOS ONE (2013) 8(6): e66247.

NAADP mediated calcium signalling and arrhythmias in the heart evoked by β-adrenergic stimulation

M Nebel, A Schwörer, D Warszta, C C Siebrands, A-C Limbrock, J M Swarbrick, R Fliegert,  M Hohenegger, A Geisler, L Herich, S Schlegel, L Carrier, T Eschenhagen, B V L Potter,  H Ehmke, and A H Guse  J Biol Chem  (2013) 288(22), 16017-16030  [JBC Paper of the Week].

Design and  synthesis of cyclic ADP-4-thioribose as a stable equivalent of cyclic ADP-ribose, a Ca²⁺-mobilizing second messenger

T Tsuzuki, N  Sakaguchi, T  Kudoh, S  Takano, M Uehara, T Murayama, T Sakurai, M Hashii, H Higashida, K Weber, A H Guse, T Kameda,  T Hirokawa, Y Kumaki, B V L Potter, H Fukuda, M Arisawa, and Shuto Angew Chem Int Edn (2013) 52(26) 6633–6637.

The Structural Biology of Estrogen Metabolism

M P Thomas and B V L Potter  J Steroid Biochem Mol Biol (2013) 137, 27-49.

Synthesis and biological evaluation of derivatives of dual aromatase-sulfatase inhibitor 4-(((4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)phenyl sulfamate

L W L Woo, P M Wood, C Bubert,  M P Thomas,  A Purohit, and B V L Potter ChemMedChem (2013) 8, 779 – 799.

STX2171, a 17b-hydroxysteroid dehydrogenase Type 3 (17b-HSD3) inhibitor, is efficacious in vivo in a novel hormone-dependent prostate cancer model

J M Day, PA Foster, H J Tutill, F. Schmidlin, J D Hargrave, N Vicker, B V L Potter, M J Reed and A Purohit Endocrine-Related Cancer (2013) 20, 563-64.

Inframolecular acid-base and coordination properties towards Na⁺ and Mg²⁺ of  myo-inositol 1,3,4,5,6-pentakisphosphate: structural approach to biologically relevant species

N Veiga,  Torres, I Macho, K  Gómez, H Y Godage, A M Riley, B V L Potter, G González and  Kremer Dalton Trans  (2013) 42, 6021-6032.

Subtype-selective regulation of IP₃ receptors by thimerosal via cysteine residues within the IP₃-binding core and suppressor domain

S ALi Khan, A M Rossi, A M Riley, B V L Potter and C W Taylor Biochem J (2013) 451, 177-184.

Regioselective opening of myo-inositol orthoesters: mechanism and synthetic utility

H Y Godage, A M Riley, T J Woodman. M P Thomas, M F Mahon & B V L Potter J Org Chem (2013) 78, 2275−2288  [Featured Article].

Stimulation of Inositol 1,4,5-trisphosphate (IP₃) receptor subtypes by Adenophostin A and its analogues

H Saleem, S C Tovey, A M.Riley, B V L Potter and C WTaylor PLOS ONE (2013) 8, e58027 1-12.

Stimulation of inositol 1,4,5-trisphosphate (IP₃) receptor subtypes by analogues of IP₃

H Saleem, S C Tovey, T Rahman, A M Riley, B V L Potter and C W Taylor  PLOS ONE (2013) 8, e54877, 1-14.

2012

First synthetic analogues of diphosphoinositol polyphosphates: interaction with PPIP5 kinase

A M Riley, H Wang, J D Weaver, S B Shears and B V L Potter Chem Comm (2012)  48, 11261-11368 [with journal front cover feature]

Adamantyl carboxamides and acetamides as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors

X Su, H A Halem, M P Thomas, C Moutrille, M D Culler, N Vicker and B V L Potter  Bioorg Med Chem (2012) 20,6394-6402.

Fibrinogen – a possible extracellular target for inositol phosphates

T Grint, A M Riley, S J Mills, B V L Potter and S T Safrany Messenger (2012) 1, 160-166.

Multivalent benzene polyphosphate derivatives are non-Ca²⁺-mobilizing Ins(1,4,5)P₃ receptor antagonists

S J Mills, T Luyten, C Erneux, J B Parys and B V L Potter Messenger (2012) 1, 167-181.

Synthesis and evaluation of thiadiazole derivatives as selective 11β-hydroxysteroid dehydrogenase type 1 inhibitors

F Pradaux-Caggiano, X Su, N Vicker, M P Thomas, D Smithen, H A Halem, M D Culler and B V L  Potter  MedChemComm (2012) 3, 1117-1124.

Determination  of neo- and d-chiro-inositol hexakisphosphate in soils by solution ³¹P NMR spectroscopy

B L Turner, A W Cheeseman,  H Y Godage, A M. Riley and B V L Potter  ACS Environmental Sci Tech (2012) 46, 4994-5002.

See also: Response to ‘Comment on “Determination of neo- and d-chiro-inositol hexakisphosphate in soils by solution ³¹P NMR spectroscopy”’

B L Turner, A W Cheesman, H Y Godage, A M. Riley, B VL Potter Environmental Sci Tech (2012) 46, 11480-11481

A synthetic polyphosphoinositide headgroup surrogate in complex with SHIP2  reveals options for drug discovery.

S J Mills, C Persson, G Cozier, M P Thomas, L Trésaugues, C Erneux, A M Riley, P Nordlund and B V L Potter ACS Chem Biol (2012) 7, 822−828.

Synthesis and evaluation of A-ring modified analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors.

L W L Woo, B Leblond, A  Purohit and B V L Potter  Bioorg Med Chem (2012) 20, 2506–2519.

An Aberrant Cyclization Affords a Cyclic Adenosine 5¢-Diphosphoribose Analog Modified at C-6 with Biological Activity in Jurkat T Cells.

C Moreau, T Kirchberger, M P Thomas, K Weber, A H  Guse and  B V L Potter J Med Chem (2012)  55, 1478-1489.

Total Synthesis of a Cyclic Adenosine 5′-Diphosphate Ribose Receptor Agonist.

J M Swarbrick and B V L Potter J Org Chem (2012) 77, 4191-4197  [Featured Article, with journal front cover design].

Contribution of Phosphates and Adenine to the Potency of Adenophostins at the InsP₃ Receptor: Synthesis of all Possible Bisphosphates of Adenophostin A.

K M Sureshan, A M Riley, S C Tovey, C W Taylor and B V L Potter J Med Chem (2012) 55, 1706-1720.

Steroidomimetic tetrahydroisoquinolines for the design of new microtubule disruptors

M P  Leese, W Dohle, F Jourdan, M Kimberley, R Bai, E Hamel, E Ferrandis and B V L Potter ACS MedChemLett (2012) 3, 5-9.

2011

[VIP paper with journal cover feature]

Development of Steroid Sulfatase Inhibitors.

L W L Woo, A Purohit and B V L Potter, Mol Cell Endocrinol (2011) 340, 175-185.

2010

Selective Determinants of IP₃ and Adenophostin A Interactions with Type 1 IP₃ Receptors.
A M Rossi, K M Sureshan, A M Riley, B V L Potter & C W Taylor, Brit J Pharmacol (2010) 161, 1070–1085.

Bicyclic derivatives of the potent Dual Aromatase-Steroid Sulfatase Inhibitor 2-bromo-4-(((4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)phenyl sulfamate: Synthesis, SAR, Crystal Structure, in vitro and in vivo Activities.
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 B V L Potter, Chem MedChem (2010) 5, 1577-1593.

NAADP mediated Ca²⁺ signaling in effector cells regulates autoimmunity of the nervous system.
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 V L Potter, A H Guse and A Flügel, Brain (2010) 133, 1930–1943.

Discovery of adamantyl ethanone derivatives as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
X Su, F Pradaux-Caggiano, M P Thomas, M Szeto, H Halem, M D Culler, N Vicker, and B V L Potter, ChemMedChem (2010) 7, 1026-1044.

Structures of four human carbonic anhydrase II/inhibitor complexes reveal a second binding site for steroidal and non-steroidal inhibitors.
G Cozier, MP Leese, M D Lloyd, M Baker, N Thiyagarajan, K R Acharya and B V L Potter Biochemistry (2010) 49,3464-3476.

Binding of IP₃ and Adenophostin A to the N-terminal Region of the IP₃ Receptor: Thermodynamic Analysis Using Fluorescence Polarization with a Novel IP₃ Receptor Ligand.
S Z Ding, A M Rossi, A M Riley, T Rahman, B V L Potter and C W Taylor, Mol Pharmacol. (2010) 77, 995-1004.

Chimeric Microtubule Disruptors.
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 V L Potter, Chem Comm (2010) 46, 2907-2909.
Highlights in Chemical Biology April 2010  and Front cover feature
ChemComm Cover feature

Synthesis, Antitubulin and Anti-proliferative SAR of Analogues of 2-Methoxy-estradiol-3,17-O,O-bissulfamates.
F Jourdan, M P Leese, W Dohle, E Hamel, E Ferrandis, S P Newman, A Purohit, M J Reed and B V L Potter, J Med Chem (2010) 53, 2942-2951.

Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
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 V L Potter, J Med Chem (2010) 53, 2155-2170.

A novel inhibitor of the PI3K/Akt pathway based on the structure of inositol 1,3,4,5,6 pentakisphosphate.
M Falasca, D Chiozzotto, H Y Godage, M Mazzoletti, A M Riley, S Previdi, B V L Potter, M Broggini and T Maffucci, Brit J Cancer (2010) 102, 104-114.

Class III beta-tubulin expression and in vitro resistance to microtubule targeting agents.
C Stengel, S P Newman, M P Leese, B V L Potter, M J Reed and A Purohit, Brit J Cancer (2010) 102, 316-324.

2009

Structural Basis for Enzymatic Evolution from a Dedicated ADP-ribosyl cyclase to a Multiple Functional NAD Hydrolase.
Q Liu, R Graeff, I A Kriksunov, H Jiang, B Zhang, N Oppenheimer, H Lin, B V L Potter, H C Lee and Q Hao, J Biol Chem (2009) 284(40), 27637-27645.

The behaviour of inositol 1,3,4,5,6-pentakisphosphate in the presence of the major biological metal cations.
N Veiga, J Torres, H Y Godage, A M Riley, S Domínguez, B V L Potter, A Díaz and C Kremer, J Biol Inorg Chem (2009) 14, 1001-1013.

Determination of the absolute configuration of aromatase and dual aromatase-sulfatase inhibitors by vibrational and electronic circular dichroism spectral analysis.
S Abbate, G Longhi, E Castiglioni, F Lebon, P M Wood, L W L Woo and B V L Potter, Chirality (2009) 21, 802-808.

Synthetic partial agonists reveal key steps in IP₃ receptor activation.
A M Rossi, A M Riley, S C Tovey, T Rahman, O Dellis, E J A Taylor, V G Veresov,  B V L Potter and C W Taylor, Nature Chem Biol (2009) 5(9), 631-639.

8-Bromo-cyclic inosine diphosphoribose: towards a selective cyclic ADP-ribose agonist.
T Kirchberger, C Moreau, G K Wagner, R Fliegert, C C Siebrands, M Nebel, F Schmid, A Harneit, F Odoardi, A Flügel, B V L Potter and A H Guse, Biochem J (2009) 422, 139–149. 

NAADP mediated Ca²⁺ signaling via type 1 ryanodine receptor in T cells revealed by a synthetic NAADP antagonist.
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 V L Potter,
Proc Natl Acad Sci USA (2009) 106, 10678-10683.

The development of steroid sulfatase inhibitors for hormone-dependent cancer therapy.
J M Day, A Purohit, H J Tutill, P A Foster, L W L Woo, B V L Potter and M J Reed, Ann NY Acad Sci (2009) 1155, 80–87.

Activation of IP₃ receptors by synthetic bisphosphate ligands. 
K M Sureshan, A M Riley, A M Rossi, S C Tovey, S G Dedos, C W Taylor and B V L Potter, Chem Comm (2009) 1204-1206.  

Discovery of Adamantyl Amides as Novel Selective Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1.
X Su, N Vicker, M Trusselle, H Halem, M Culler and B V L Potter, Mol Cell Endocrinol (2009) 301, 169-173.

The Design of Novel 17β-Hydroxysteroid Dehydrogenase Type 3 Inhibitors.
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 V L Potter, Mol Cell Endocrinol (2009) 301, 259-265. 

Development of hormone-dependent prostate cancer models for the evaluation of inhibitors of 17β-hydroxysteroid dehydrogenase Type 3.
J M Day, H J Tutill, P A Foster, H V Bailey, W B Heaton, C M Sharland, N Vicker, B V L Potter, A Purohit and M J Reed, Mol Cell Endocrinol (2009) 301, 251-258.  

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.
J M Day, P A Foster, H J Tutill, S P Newman, Y T Ho, M P Leese, B V L Potter, M J Reed and A Purohit, Brit J Cancer (2009) 100, 476-486.  
 

2008

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 V L Potter, M J Reed, A Purohit and S P Newman, Brit J Cancer (2008) 99, 1842-1848.  

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.
F Jourdan , C Bubert , M P Leese, A Smith , E Ferrandis, S Regis-Lydi, S P Newman, A Purohit, M J Reed and B V L Potter, Org Biomol Chem (2008) 6, 4108-4119.

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.
C Bubert, L W L Woo, O Sutcliffe, M F Mahon, S K Chander, A Purohit, M J Reed and B V L Potter, ChemMedChem (2008) 3, 1708-1730.

The in vivo properties of STX243: a potent angiogenesis inhibitor.
M F C Parsons, P A Foster, S K Chander, R Jhalli, S P Newman, M P Leese, B V L Potter, A Purohit and M J Reed, Brit J Cancer (2008) 99, 1433-1441.

A new therapeutic strategy against hormone-dependent breast cancer: The preclinical development of a dual aromatase and sulfatase inhibitor.
P A Foster, S K Chander, S P Newman, L W L Woo, O B Sutcliffe, C Bubert, D Zhou, S Chen, B V L Potter, M J Reed and A Purohit, Clin Cancer Res (2008) 14(20), 6469-6477.

The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone dependent endometrial cancer. Steroid sulfatase inhibitors and endometrial cancer.
P A Foster, L W L Woo, B V L Potter, M J Reed and A Purohit, Endocrinology (2008) 149, 4035-4032.

Efficacy of three potent steroid sulfatase inhibitors: Pre-clinical investigations for their use in the treatment of hormone-dependent breast cancer.
P A Foster, S K Chander, M Parsons, S P Newman, R Jhalli, L W L Woo, B V L Potter, M J Reed and A Purohit, Breast Cancer Res Treat (2008) 111, 129-138.

2-MeOE2bisMATE and 2-EtE2bisMATE induce cell cycle arrest and apoptosis in breast cancer xenografts as shown by a novel ex vivo technique.
P A Foster, Y T Ho, B Raobaikady, S P Newman, P G Kasprzyk, M P Leese, B V L Potter, M J Reed and A Purohit, Breast Cancer Res Treat (2008) 111, 251-260.

Design and synthesis of 4”,6”-unsaturated cyclic ADP-carbocyclic ribose, a Ca2+-mobilizing agent selectively active in T cells.
T Kudoh, T Murayama, M Hashii, H Higashida, T Sakurai, C Maechling, B Spiess, K Weber, A H Guse, M Arisawa, B V L Potter, A Matsuda and S Shuto, Tetrahedron (2008) 64, 9754-9765.

Steroid sulphatase inhibitors as a target for the topical treatment of skin disorders.
M J Reed, A Purohit, L W L Woo and B V L Potter (2008) Drugs Future 33(7), 597-606.

Benzene Polyphosphates as tools for cell signaling: interaction with the PH domain of protein kinase Ba and inhibition of inositol 1,4,5-trisphosphate 5-phosphatase.
S J Mills, F Vandeput, M N Trusselle, S T Safrany, C Erneux and B V L Potter ChemBioChem (2008) 9,1757-1766.

Chiral Aromatase and Dual Aromatase-Steroid Sulfatase Inhibitors from the Letrozole Template: Synthesis, Absolute Configuration and In Vitro Activity.
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 B V L Potter, J Med Chem (2008) 51, 4226-4238.

Anti-cancer steroid sulfatase inhibitors: synthesis, in vitro and in vivo activities, molecular modelling and protein crystallography of a potent fluorinated second-generation agent.
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 B V L Potter, Mol Cancer Ther (2008) 7(8), 2435-2444.

Inhibition of steroid sulphatase activity in endometriotic implants by 667COUMATE: a potential new therapy.
A Purohit, L Fusi, J Brosens, D Parish, M S Fernandes, L W L Woo, B V L Potter and M J Reed. Human Reproduction (2008) 23, 290-297.

STX140 is efficacious in vitro and in vivo in taxane resistant breast carcinoma cells.
S P Newman, P A Foster, C Stengel, J M Day, Y T Ho, J-G Judde, M Lassalle, G Prevost, M P Leese, B V L Potter, M J  Reed and A Purohit. Clin Cancer Res (2008) 14(2), 597-606.

Direct Evidence for ArO-S Bond Cleavage upon Inactivation of Pseudomonas aeruginosa Arylsulfatase by Aryl Sulfamates.
P Bojarova, E Denehy, I Walker, K Loft, D P De Souza, L W L Woo, B V L Potter, M J McConville and S J Williams. ChemBioChem (2008) 9, 613 – 623.

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.
K M Sureshan, M Trusselle, S C Tovey, C W Taylor and B V L Potter, J Org Chem (2008) 73, 1682-1692  [JOC Featured Article].

Chemoenzymatic synthesis of 7-deaza cyclic adenosine 5'-diphosphate ribose analogues, membrane permeant modulators of intracellular calcium release.
B Zhang, V C Bailey and B V L Potter, J Org Chem (2008) 73, 1693-1703.

17ß-Hydroxysteroid dehydrogenase type 1 and not type 12 is a target for endocrine therapy of hormone-dependent breast cancer.
 J M Day, S P Newman, Y T Ho, P A Foster, M P Leese, B V L Potter, M J Reed and A Purohit, Int J Cancer (2008) 122, 1931-1940.

2'-Deoxy Cyclic Adenosine 5'-Diphosphate Ribose Derivatives: Importance of a 2' Hydroxyl Motif for the Antagonistic Activity of 8-Substituted cADPR Derivatives.
B Zhang, G Wagner, K Weber, C Garnham, A Morgan, A Galione, A H Guse and B V L Potter, J Med Chem (2008) 51, 1623–1636.

Structure-Activity Relationships of C-17 Cyanated Estratrienes as Anti-cancer agents.
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 B V L Potter, J Med Chem (2008) 51, 1295–1308.

Inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1.
X Su, N Vicker and B V L Potter, Prog Med Chem (2008) 46, 29-130.

Novel Non-steroidal Aromatase Inhibitors Based On a Biphenyl Scaffold: synthesis, in vitro SAR and molecular modelling.
T Jackson, L W L Woo, M N Trusselle, A Purohit, M J Reed and B V L Potter, Chem Med Chem (2008) 3, 603-618.

Novel Inhibitors of 17ß Hydroxysteroid Dehydrogenase Type 1: Templates for Design.
G M Allan, N Vicker, H R Lawrence, H J Tutill, J M Day, M Huchet, E Ferrandis, M J Reed, A Purohit and B V L Potter, Bioorg Med Chem (2008) 16, 4438–4456.

2007

The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers.
S P Newman, P A Foster, Y T Ho, J M Day, B Raobaikady, P G Kasprzyk, M P Leese, B V L Potter, M J Reed and A Purohit. Brit J Cancer (2007) 97, 1673 - 1682.

Dual aromatase-sulfatase inhibitors based on the anastrozole template: synthesis, in vitro SAR, molecular modelling and in vivo activity.
T Jackson, L W L Woo, M N Trusselle, S K Chander, A Purohit, M J Reed and B V L Potter, Org & Biomol Chem (2007) 5, 2940-2952.

Catalysis associated conformational changes revealed by human CD38 complexed with a non-hydrolyzable substrate analog.
Q Liu, I A Kriksunov, C Moreau, R Graeff, B V L Potter, H C Lee and Q Hao, J Biol Chem (2007) 282, 24825-24832.

3,17-Disubstituted 2-alkyestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anti-cancer activity.
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 V L Potter, J Med Chem (2007) 50, 4431-4443.

Dual aromatase-steroid sulfatase inhibitors.
L W L Woo, C Bubert, O B Sutcliffe, A Smith, S K Chander, M F Mahon, A Purohit, M J Reed and B V L Potter, J Med Chem (2007) 50, 3540-3560.

Novel inositol phospholipid headgroup surrogate crystallised in the PH domain of protein kinase Ba.
S J Mills, D Komander, M N Trusselle, D M F van Aalten and B V L Potter, ACS Chem Biol (2007) 2 (4), 242-246. Cover feature

Nicotinamide 2-fluoroadenine dinucleotide unmasks the NAD⁺ glycohydrolase activity of Aplysia Californica adenosine 5'-diphosphate-ribosyl cyclase.
B Zhang, H Muller-Steffner, F Schuber and B V L Potter, Biochemistry (2007) 46, 4100-4109.

Biphenyl-2,3’4,5’,6-pentakisphosphate, a novel inositol polyphosphate surrogate, inhibits the activity of two inositide 5-phosphatases and modulates Ca²⁺ responses in rat hepatocytes.
F Vandeput, L Combettes, S J Mills, K Backers, A Wohlkonig, J Parys, H De Smedt, L Missiaen, G Dupont, B V L Potter and C Erneux, FASEB J (2007) 21, 1481-1491.

Rapid and efficient routes to phosphatidylinositol 3,4,5-trisphosphates via myo-inositol orthobenzoate.
K M Sureshan, A M Riley and B V L Potter, Tet Lett (2007) 48 1923-1926.

2006

2-Substituted estradiol bis-sulfamates, multi-targeted anti-tumor agents: Synthesis, in vitro SAR, protein crystallography and in vivo activity.
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 V L Potter, J Med Chem (2006) 49, 7683-7696.

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.
S J Mills, H Dozol, F Vandeput, K Backers, T Woodman, C Erneux, B Spiess and B V L Potter, Chem Biochem (2006) 7, 1696-1706.

Cellular effects and metabolic stability of N1-cyclic inosine diphosphoribose and its derivatives.
T Kirchberger, G Wagner, J Xu, P Wang, A Gasser, R Fliegert, S Bruhn, F E Lund, L-H Zhang, B V L Potter and A H Guse, Brit J Pharmacol, (2006) 149, 337-344.

A Systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Synthesis of -C-glucoside trisphosphates based on the conformational restriction strategy.
M Terauchi, H Abe, S C Tovey, S G Dedos, C W Taylor, M Paul, M Trusselle and B V L Potter, A Matsuda and S Shuto, J Med Chem (2006) 49, 1900-1909.

Design and synthesis of 5'-deoxy-5'-phenyladenophostin A, a highly potent IP3 receptor ligand.
T Mochizuki, Y Kondo, H Abe, C W Taylor, B V L Potter, A Matsuda and S Shuto, Org Letts (2006) 8 (7), 1455-1458.

Focused libraries of 16 substituted estrone derivatives and modified E-ring steroids: Inhibitors of 17 -hydroxysteroid dehydrogenase type 1.
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 B V L Potter, Chem Med Chem (2006) 1, 464-481.

Guanophostin A: Synthesis and evaluation of a high affinity agonist of the D-myo-inositol 1,4,5 trisphosphate receptor.
K M Sureshan, M Trusselle, S C Tovey, C W Taylor and B V L Potter, Chem Comm (2006) 2015-2017.

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.
H Y Godage, A M Riley, T J Woodman and B V L Potter, Chem Comm (2006) 2989-2991.

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.
C Moreau, G K Wagner, K Weber, A H Guse and B V L Potter, J Med Chem (2006) 49, 5162-5176.

Cell-permeant small-molecule modulators of NAADP-mediated Ca²⁺ release.
J Dowden, G Berridge, C Moreau, M Yamasaki, G C Churchill, B V L Potter and A Galione, Chemistry & Biology (2006) 13, 659-665.

Rapid microwave-assisted reductive amination of ketones with anilines.
H V Bailey, W Heaton, N Vicker and B V L Potter, SynLett (2006) 15, 2444-2448.

scyllo-Inositol pentakisphosphate as an analogue of myo-inositol 1,3,4,5,6-pentakisphosphate: chemical synthesis, physicochemistry and biological applications.
A M Riley, M Trusselle, P Kuad, M Borkovec, J Cho, J Choi, X Qian, S B Shears, B Spiess and B V L Potter, Chem Bio Chem (2006) 7, 1114-1122.

In vivo efficacy of STX213, a second generation steroid sulfatase inhibitor for hormone-dependent breast cancer therapy.
P A Foster, S P Newman, S K Chander, C Stengel, R Jhalli, L W L Woo, B V L Potter, M J Reed and A Purohit, Clin Cancer Res (2006) 12, 5543-5549.

Synthesis of Adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP₃ receptor ligands.
T Mochizuki, Y Kondo, H Abe, A Matsuda, S Shuto, S C Tovey, S G Dedos, C W Taylor, M Paul and B V L Potter, J Med Chem (2006) 49, 5750-5758.

Phase I study of STX64 (667 Coumate) in breast cancer patients: the first study of a steroid sulphatase inhibitor.
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, B V L Potter, M J Reed and R C Coombes Clin Cancer Res (2006) 12 (5) 1585-1592.

On the contribution of stereochemistry to ITPK1 specificity: Ins(1,4,5,6)P4 is not a physiologic substrate.
A M Riley, S Deleu, X Qian, J Mitchell, S-K Chung, S Adelt, G Vogel, B V L Potter and S B Shears, FEBS Lett (2006) 324-330.

Chiral desymmetrisation of myo-inositol 1,3,5-orthobenzoate gives rapid access to precursors for second messenger analogues.
A M Riley, H Y Godage, M F Mahon and B V L Potter, Tetrahedron Asymmetry (2006) 17, 171-174.

Modification of estrone at the 6, 16, 17 positions: Novel potent inhibitors of 17 -hydroxysteroid dehydrogenase type 1.
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 B V L Potter, J Med Chem (2006) 49, 1325-1345.

Unusual entry to the novel 8-halo-N1-ribosyl hypoxanthine system by degradation of a cyclic adenosine-5'-diphosphate ribose analogue.
C Moreau, T J Woodman and B V L Potter, Chem Comm (2006) 1127-1129.

2005

Steroid sulfatase: Molecular biology, regulation and inhibition
M J Reed, A Purohit, L W L Woo, S P Newman and B V L Potter, Endocrine Reviews (2005) 26 (2), 171-202.

Crystal structure of human carbonic anhydrase II at 1.95 Å resolution in complex with 667-coumate, a novel anti-cancer agent.
M D Lloyd, R L Pederick, R Natesh, L W L Woo, A Purohit, M J Reed, K R Acharya and B V L Potter, Biochem J (2005) 385, 715-720.

Adenophostin A and analogues modified at the adenine moiety: synthesis, conformational analysis and biological activity.
C N Borissow, S J Black, M Paul, S C Tovey, S G Dedos, C W Taylor and B V L Potter, Org Biomol Chem (2005) 3, 245-252.

First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors.
M D Lloyd, N Thiyagarajan, Y T Ho, L W L Woo, O B Sutcliffe, A Purohit, M J Reed, K R Acharya and B V L Potter, Biochemistry (2005) 44, 6858-6866.

Novel and potent 17 -hydroxysteroid dehydrogenase type 1 inhibitors.
H R Lawrence, N Vicker, G M Allan, A Smith, M F Mahon, H J Tutill, A Purohit, M J Reed and B V L Potter, J Med Chem (2005) 48, 2759-2762.

Rapid synthetic route towards structurally modified derivatives of cyclic adenosine 5'-diphosphate ribose.
G K Wagner, A H Guse and B V L Potter, J Org Chem (2005) 70, 4810-4819.

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.
T Kudoh, M Fukuoka, S Ichikawa, T Murayama, Y Ogawa, M Hashii, H Higashida, S Kunerth, K Weber, A H Guse, B V L Potter, A Matsuda and S Shuto, J Amer Chem Soc (2005) 127, 8846-8855.

Interaction of the catalytic domain of Inositol 1,4,5-trisphosphate 3-kinase A with inositol phosphate analogues.
A Poinas, K Backers, A M Riley, S J Mills, C Moreau, B V L Potter and C Erneux, Chem Biochem (2005) 6, 1449-1457.

A-ring substituted estrogen-3-O-sulfamates: Potent multi-targeted anti-cancer agents.
M P Leese, H A M Hejaz, M F Mahon, S P Newman, A Purohit, M J Reed and B V L Potter, J Med Chem (2005) 48, 5243-5256.

E-Ring modified steroids as novel potent inhibitors of 17 -hydroxysteroid dehydrogenase type 1.
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 B V L Potter, J Med Chem (2005) 48, 5749-5770.pp 

Inhibition of the Phosphatidylinositol 3-kinase/Akt pathway by inositol pentakisphosphate results in antiangiogenic and antitumour effects.
T Maffucci, E Piccolo, A Cumashi, M Iezzi, A M Riley, A Saiardi, H Y Godage, C Rossi, M Broggini, S Iacobelli, B V L Potter, P Innocenti and M Falasca, Cancer Research (2005) 65, 8339-8349.

2004

Inhibition of in vitro angiogenesis by 2-methoxy- and 2-ethyl-estrogen sulfamates.
S P Newman, M P Leese, A Purohit, D R C James, C E Rennie, B V L Potter and M J Reed, Int J Cancer (2004) 109, 533-540.

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.
F Abbate, J-Y Winum, B V L Potter, A Casini, J-L Montero, A Scozzafava and C T Supuran, Bioorg Med Chem Lett (2004) 14, 231-234.

Inositol pentakisphosphate promotes apoptosis through the PI 3-K/Akt pathway.
E Piccolo, S Vignati, T Maffucci, P F Innominato, A M Riley, B V L Potter, P P Pandolfi, M Broggini, S Iacobelli, P Innocenti and M Falasca, Oncogene (2004) 23, 1754-1765.

Dimers of D-myo-inositol 1,4,5-trisphosphate: Design, synthesis and interaction with Ins(1,4,5)P3 receptors.
A M Riley, A J Laude, C W Taylor and B V L Potter, Bioconjugate Chem (2004) 15, 278-289.

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.
A M Riley, H Dozol, B Spiess and B V L Potter, Biochem Biophys Res Comm (2004) 318, 444-452.

2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents.
M P Leese, S P Newman, A Purohit, M J Reed and B V L Potter, Bioorg Med Chem Lett (2004) 14, 3135-3138.

2-MeOE2bisMATE induces caspase-dependent apoptosis in CAL51 breast cancer cells and overcomes resistance to TRAIL via cooperative activation of caspases.
L Wood, M P Leese, A Mouzakiti, A Purohit, B V L Potter, M J Reed and G Packham, Apoptosis (2004) 9, 323-332.

Amplification and propagation of pacemaker Ca2+ signals by cyclic ADP-ribose and the type 3 ryanodine receptor in T cells.
S Kunerth, M F Langhorst, N Schwarzmann, X Gu, L Huang, Z Yang, L Zhang, S J Mills, L-H Zhang, B V L Potter and A H Guse, J Cell Sci (2004) 117, 2141-2149.

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.
R B Gregory, R Hughes, A M Riley, B V L Potter, R A Wilcox and G J Barritt, Biochem J (2004) 381, 519-526.

Novel 18 -Glycyrrhetinic acid analogues as potent and selective inhibitors of 11 -hydroxysteroid dehydrogenases.
X Su, H Lawrence, D Gaheshapillai, A Cruttenden, A Purohit, M J Reed, N Vicker and B V L Potter, Bioorg Med Chem (2004) 12, 4439-4457.

Chemical synthesis of the second messenger nicotinic acid adenine dinucleotide phosphate by total synthesis of nicotinamide adenine dinucleotide phoshate.
J Dowden, C Moreau, R S Brown, G Berridge, A Galione and B V L Potter, Angewandte Chemie Int Edn (2004) 43, 4637-4640.

Regulation of casein kinase-2 (CK2) activity by inositol phosphates.
L Solyakov, K Cain, B M Tracey, R Jukes, A M Riley, B V L Potter, A B Tobin, J Biol Chem (2004) 279, 43403-43410.

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.
G Horne, C Maechling, A Fleig, M Hirata, R Penner, B Spiess and B V L Potter, Biochem Biophys Res Comm (2004) 320, 1262-1270.

Aplysia californica mediated cyclisation of novel 3'-modified NAD analogues: A role for hydrogen bonding in the recognition of cyclic adenosine 5'-diphosphate ribose.
C J W Mort, M E Migaud, A Galione and B V L Potter, Bioorg Med Chem, (2004) 12, 475-487.

2003

Synthesis and Ca²⁺ mobilising activity of purine-modified mimics of adenophostin A: A model for the adenophostin-Ins(1,4,5)P3 receptor interaction.
H J Rosenberg, A M Riley, A J Laude, C W Taylor and B V L Potter, J Med Chem (2003) 46, 4860-4871.

Identification of mammalian Vps24p as an effector of phosphatidylinositol 3,5 bisphosphate-dependent endosome compartmentalization.
P Whitley, B J Reaves, M Hashimoto, A M Riley, B V L Potter and G D Holman, J Biol Chem (2003) 278, 38786-38795.

Convergent synthesis and unexpected Ca²⁺-mobilizing activity of the 8-substituted analogues of cyclic ADP-carbocyclic ribose, a stable mimic of Ca²⁺-mobilizing second messenger cyclic ADP-ribose.
S Shuto, M Fukuoka, T Kudoh, C Garnham, A Galione, B V L Potter and A Matsuda, J Med Chem (2003) 46, 4741-4749.

First enzymatic synthesis of an N1-cyclised cADPR (cyclic-ADP ribose) analogue with an hypoxanthine partial structure: discovery of a membrane permeant cADPR agonist.
G K Wagner, S Black, A H Guse and B V L Potter, Chem Comm (2003) 1944-1945.

First dual aromatase-steroid sulfatase inhibitor.
L W L Woo, C Bubert, O B Sutcliffe, A Grasso, S Chander, A Purohit, M J Reed and B V L Potter, J Med Chem (2003) 46, 3193-3196.

D-ring modified estrone derivatives as novel potent inhibitors of steroid sulfatase.
D S Fischer, L W L Woo, M F Mahon, A Puroit, M J Reed and B V L Potter, Bioorg Med Chem (2003) 11, 1685-1700.

2002

Estrone 3-sulfate mimics, inhibitors of estrone sulfatase activity: Homology model construction and docking studies
N M Howarth, A Purohit, J J Robinson, N Vicker, M J Reed and B V L Potter, Biochemistry (2002) 41, 14801-14814.

Interactions of inositol 1,4,5-trisphosphate receptors with synthetic poly(ethylene glycol)-linked dimmers of IP₃ suggest close spacing of the IP₃-binding sites.
A M Riley, S A Morris, E P Nerou, V Correa, B V L Potter and C W Taylor, J Biol Chem (2002) 277, 40290-40295.

Novel hydrolysis-resistant analogues of cyclic ADP-ribose: Modification of the "northern" ribose and calcium release activity.
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 B V L Potter, Biochemistry (2002) 41, 6744-6751.

Regulation of Ins(3,4,5,6)P₄ signaling by a reversible kinase/phosphatase.
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, B V L Potter and S B Shears, Current Biology (2002) 12, 477-482.

2001

Total synthesis of nucleobase-modified adenophostin A mimics.
S Shuto, G Horne, R D Marwood and B V L Potter, Chemistry - A European Journal, (2001) 7, 4937-4946.

Bicyclic analogs of D-myo-inositol 1,4,5-trisphosphate related to adenophostin A: Synthesis and biological activity.
A M Riley, V Correa, M F Mahon, C W Taylor and B V L Potter, J Med Chem, (2001) 44, 2108-2117.

Structural determinants of adenophostin A activity at inositol trisphosphate receptors.
V Correa, A M Riley, S Shuto, G Horne, E P Nerou, R D Marwood, B V L Potter and C W Taylor, Mol Pharmacol (2001) 59, 1206-1215.

2000

Nicotinic acid adenine dinucleotide phosphate (NAADP⁺) is an essential regulator of T-lymphocyte Ca²⁺-signaling.
I Berg, B V L Potter, G W Mayr and A H Guse, J Cell Biol (2000) 150, 581-588.

Synthesis of potent agonists of the D-myo-inositol 1,4,5-trisphosphate receptor based on clustered disaccharide polyphosphate analogues of adenophostin A.
M de Kort, V Correa, A R P M Valentijn, G A van der Marel, B V L Potter, C W Taylor and J H van Boom, J Med Chem (2000) 43, 3295-3303.

InsP₄ facilitates store-operated calcium influx by inhibition of InsP₃ 5-phosphatase.
M C Hermosura, H Takeuchi, A Fleig, A M Riley, B V L Potter, M Hirata and R Penner, Nature (2000) 408, 735-740.

1999

Structure of the PH domain from Bruton's tyrosine kinase in complex with inositol 1,3,4,5-tetrakisphosphate.
E Baraldi, K D Carugo, M Hyvönen, P L Surdo, A M Riley, B V L Potter, R O'Brien, J E Ladbury and M Saraste, Structure (1999) 7, 449-460.

Regulation of calcium signalling in T lymphocytes by the second messenger cyclic ADP-ribose.
A H Guse, C P da Silva, I Berg, A L Skapenko, K Weber, P Heyer, M Hohenegger, G A Ashamu, H Schulz-Koops, B V L Potter and G W Mayr, Nature (1999) 398, 70-73.

Evidence of a role for cyclic ADP-ribose in long-term synaptic depression in hippocampus.
M Reyes-Harde, R Empson, B V L Potter, A Galione and P K Stanton, Proc Natl Acad Sci USA (1999) 96, 4061-4066.

1998

Steroidal and non-steroidal sulfamates as potent inhibitors of steroid sulfatase.
L W L Woo, N M Howarth, A Purohit, H A M Hejaz, M J Reed and B V L Potter, J Med Chem (1998) 41, 1068-1083.

A conformationally restricted cyclic phosphate analogue of inositol trisphosphate: synthesis and physicochemical properties
A M Riley, P Guédat, G Schlewer, B Spiess and B V L Potter, J Org Chem (1998) 63, 295-305.

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.
D J Jenkins and B V L Potter, J Chem Soc Perkin Trans I (1998) 41-49.

1997

Disaccharide polyphosphates based upon adenophostin A activate hepatic d-myo-inositol 1,4,5-trisphosphate receptors.
J S Marchant, M D Beecroft, A M Riley, D J Jenkins, R D Marwood, C W Taylor and B V L Potter, Biochemistry (1997) 36, 12780-12790.

Structural analogues of D-myo- inositol 1,4,5-trisphosphate and adenophostin A: Recognition by cerebellar and platelet inositol 1,4,5-trisphosphate receptors.
C T Murphy, A M Riley, C J Lindley, D J Jenkins, J Westwick and B V L Potter, Mol Pharmacol (1997) 52, 741-748.

Rapid synthesis of the enantiomers of myo-inositol 1,3,4,5-tetrakisphosphate by direct chiral desymmetrization of myo-inositol orthoformate.
A M Riley, M F Mahon and B V L Potter, Angew Chem Int Edn Eng (1997) 36, 1472-1474.

1996

Isotopic enrichment by asymmetric deuteriation. An investigation of the synthesis of deuteriated (S)-(-)-methylsuccinic acids from itaconic acid.
D J Hardick, I S Blagbrough and B V L Potter, J Am Chem Soc (1996) 118, 5897-5903.   

Cyclic aristeromycin diphosphate ribose:  A potent and poorly hydrolysable Ca2+-mobilising mimic of cyclic adenosine diphosphate ribose.

V C Bailey, S M Fortt, R J Summerhill, A Galione and B V L Potter, FEBS Lett (1996) 379, 227-230.

Active site-directed inhibition of estrone sulfatase by non-steroidal coumarin sulfamates.

L W L Woo, A Purohit, M J Reed and B V L Potter, J Med Chem (1996) 39, 1349-1351.

Synthesis of D-2-deoxy-myo-inositol 1,3,4,5-tetrakisphosphate from D-glucose.

D J Jenkins, D Dubreuil and B V L Potter, J Chem Soc Perkin Trans I (1996) 1365-1372.

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.

D J Callis, N F Thomas, D P J Pearson and B V L Potter, J Org Chem (1996) 61, 4634-4640.

A specific cyclic ADP-ribose antagonist inhibits cardiac excitation-contraction coupling.

S Rakovic, A Galione, G A Ashamu, B V L Potter and D A Terrar, Curr Biol, (1996) 6, 989-996.

Chiral cyclopentane-based mimics of D-myo-inositol-1,4,5-trisphosphate from   D-glucose.

D J Jenkins, A M Riley and B V L Potter, J Org Chem (1996) 61, 7719-7726.