Barry Vl Potter

Summary

Affiliation: University of Bath
Country: UK

Publications

  1. pmc Synthesis of cyclic adenosine 5'-diphosphate ribose analogues: a C2'endo/syn "southern" ribose conformation underlies activity at the sea urchin cADPR receptor
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath, UK BA2 7AY
    Org Biomol Chem 9:278-90. 2011
  2. pmc Structure-activity relationship of adenosine 5'-diphosphoribose at the transient receptor potential melastatin 2 (TRPM2) channel: rational design of antagonists
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    J Med Chem 56:10079-102. 2013
  3. pmc Total synthesis of a cyclic adenosine 5'-diphosphate ribose receptor agonist
    Joanna M Swarbrick
    Wolfson Laboratory of Medicinal Chemistry, University of Bath, Department of Pharmacy and Pharmacology, Claverton Down, Bath BA2 7AY, UK
    J Org Chem 77:4191-7. 2012
  4. pmc Aberrant cyclization affords a C-6 modified cyclic adenosine 5'-diphosphoribose analogue with biological activity in Jurkat T cells
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom
    J Med Chem 55:1478-89. 2012
  5. pmc Contribution of phosphates and adenine to the potency of adenophostins at the IP₃ receptor: synthesis of all possible bisphosphates of adenophostin A
    Kana M Sureshan
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    J Med Chem 55:1706-20. 2012
  6. pmc A synthetic polyphosphoinositide headgroup surrogate in complex with SHIP2 provides a rationale for drug discovery
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, U K
    ACS Chem Biol 7:822-8. 2012
  7. pmc Regioselective opening of myo-inositol orthoesters: mechanism and synthetic utility
    Himali Y Godage
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    J Org Chem 78:2275-88. 2013
  8. pmc Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA27AY, UK
    ChemMedChem 6:1439-51. 2011
  9. pmc Aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole and vorozole templates
    Paul M Wood
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA27AY, UK
    ChemMedChem 6:1423-38. 2011
  10. pmc Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA27AY, UK
    ChemMedChem 6:1616-29. 2011

Collaborators

Detail Information

Publications101 found, 100 shown here

  1. pmc Synthesis of cyclic adenosine 5'-diphosphate ribose analogues: a C2'endo/syn "southern" ribose conformation underlies activity at the sea urchin cADPR receptor
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath, UK BA2 7AY
    Org Biomol Chem 9:278-90. 2011
    ....
  2. pmc Structure-activity relationship of adenosine 5'-diphosphoribose at the transient receptor potential melastatin 2 (TRPM2) channel: rational design of antagonists
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    J Med Chem 56:10079-102. 2013
    ..8-Ph-ADPR (5) inhibits Ca(2+) signalling and chemotaxis in human neutrophils, illustrating the potential for pharmacological intervention at TRPM2. ..
  3. pmc Total synthesis of a cyclic adenosine 5'-diphosphate ribose receptor agonist
    Joanna M Swarbrick
    Wolfson Laboratory of Medicinal Chemistry, University of Bath, Department of Pharmacy and Pharmacology, Claverton Down, Bath BA2 7AY, UK
    J Org Chem 77:4191-7. 2012
    ..We report the first total synthesis of the membrane permeant, hydrolytically stable, cADPR receptor agonist 8-Br-N1-cIDPR via regio- and stereoselective N1-ribosylation of protected 8-bromoinosine...
  4. pmc Aberrant cyclization affords a C-6 modified cyclic adenosine 5'-diphosphoribose analogue with biological activity in Jurkat T cells
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom
    J Med Chem 55:1478-89. 2012
    ....
  5. pmc Contribution of phosphates and adenine to the potency of adenophostins at the IP₃ receptor: synthesis of all possible bisphosphates of adenophostin A
    Kana M Sureshan
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    J Med Chem 55:1706-20. 2012
    ..A model with a possible adenine-R504 interaction supports the activity of 5 and 6 and also allows a reappraisal of the unexpected activity previously reported for the AdA regioisomer 2″-phospho-3″-dephospho-AdA 40...
  6. pmc A synthetic polyphosphoinositide headgroup surrogate in complex with SHIP2 provides a rationale for drug discovery
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, U K
    ACS Chem Biol 7:822-8. 2012
    ..Molecular dynamics simulations suggest that when BiPh(2,3',4,5',6)P(5) binds to SHIP2, a flexible loop folds over and encloses the ligand. Compounds targeting such a closed conformation might therefore deliver SHIP2-specific drugs...
  7. pmc Regioselective opening of myo-inositol orthoesters: mechanism and synthetic utility
    Himali Y Godage
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    J Org Chem 78:2275-88. 2013
    ..Investigation into this selective formation of 2-O-ester products and the deuterium incorporation is presented with proposed mechanisms from NMR experiments...
  8. pmc Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA27AY, UK
    ChemMedChem 6:1439-51. 2011
    ..Selected potent 11β-HSD1 inhibitors show moderate metabolic stability upon incubation with human liver microsomes and weak inhibition of human CYP450 enzymes...
  9. pmc Aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole and vorozole templates
    Paul M Wood
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA27AY, UK
    ChemMedChem 6:1423-38. 2011
    ..52 nM; STS: IC₅₀ =280 nM). The docking of each enantiomer and other ligands into the aromatase and sulfatase active sites was also investigated...
  10. pmc Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA27AY, UK
    ChemMedChem 6:1616-29. 2011
    ..The most potent inhibitors have IC₅₀ values around 34-48 nM against human 11β-HSD1, display reasonable metabolic stability in human liver microsomes, and weak inhibition of key human CYP450 enzymes...
  11. ncbi request reprint 'Click cyclic ADP-ribose': a neutral second messenger mimic
    Joanna M Swarbrick
    Wolfson Laboratory of Medicinal Chemistry, Dept of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK
    Chem Commun (Camb) 50:2458-61. 2014
    ..The ability to activate Ca(2+) release was surprisingly retained, and hydrolysis of cADPR by CD38 could also be inhibited, illustrating the potential of this approach to design drug-like signalling pathway modulators. ..
  12. pmc Adamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem 20:6394-402. 2012
    ..Importantly, compound 41 (IC(50)=280 nM) provides a new lead that incorporates an adamantyl group surrogate and should enable further series diversification...
  13. ncbi request reprint First synthetic analogues of diphosphoinositol polyphosphates: interaction with PP-InsP5 kinase
    Andrew M Riley
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, BA2 7AY, UK
    Chem Commun (Camb) 48:11292-4. 2012
    ..PA-InsPs are promising candidates for further studies into the biology of PP-InsPs...
  14. ncbi request reprint Medicinal chemistry and pharmacology of cyclic ADP-ribose
    Barry V L Potter
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Curr Mol Med 4:303-11. 2004
    ..This review will focus on the synthesis and properties of analogs that have been shown to have utility in dissecting the role of cADPR in calcium signaling...
  15. ncbi request reprint Anticancer steroid sulfatase inhibitors: synthesis of a potent fluorinated second-generation agent, in vitro and in vivo activities, molecular modeling, and protein crystallography
    L W Lawrence Woo
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, United Kingdom
    Mol Cancer Ther 7:2435-44. 2008
    ..Compound (10) and other related inhibitors of this structural class further expand the armory of steroid sulfatase inhibitors against hormone-dependent breast cancer...
  16. ncbi request reprint 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, United Kingdom
    J Med Chem 49:7683-96. 2006
    ..2-Substituted E2bisMATEs are attractive candidates for further development as multitargeted anticancer agents...
  17. ncbi request reprint Dual aromatase-steroid sulfatase inhibitors
    L W Lawrence Woo
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Limited, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    J Med Chem 50:3540-60. 2007
    ..DASI 5 did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed...
  18. ncbi request reprint Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery
    Mark P Thomas
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Future Med Chem 3:367-90. 2011
    ..However, the differences are significant for drug discovery. The crystal structures can be of use in drug discovery, but care needs to be taken when selecting structures for use in virtual screening and ligand docking...
  19. ncbi request reprint A-ring-substituted estrogen-3-O-sulfamates: potent multitargeted anticancer agents
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, U K
    J Med Chem 48:5243-56. 2005
    ..The potential of this novel class of multimechanism anticancer agents was confirmed in vivo with good activity observed in the NCI hollow fiber assay and in a MDA-MB-435 xenograft mouse model...
  20. ncbi request reprint Adenophostin A and analogues modified at the adenine moiety: synthesis, conformational analysis and biological activity
    Charles N Borissow
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, UK BA2 7AY
    Org Biomol Chem 3:245-52. 2005
    ..e. that a cation-pi interaction between the base moiety and Arg 504 of the receptor in combination with H-bonding may be responsible for the high potency of adenophostin A relative to Ins(1,4,5)P(3)...
  21. ncbi request reprint Chemical synthesis of the novel Ca2+ messenger NAADP
    James Dowden
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Nucleosides Nucleotides Nucleic Acids 24:513-8. 2005
    ..This flexible synthetic route offers new opportunities for the generation of NAADP 1 analogues that cannot be generated directly from NADP 2 or mainly enzymatic methods...
  22. doi request reprint Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template
    L W Lawrence Woo
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, UK
    J Med Chem 53:2155-70. 2010
    ..A complex was crystallized and its structure was solved by X-ray crystallography. This class of DASI should encourage further development toward multitargeted therapeutic intervention in HDBC...
  23. ncbi request reprint D-ring modified estrone derivatives as novel potent inhibitors of steroid sulfatase
    Delphine S Fischer
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Bioorg Med Chem 11:1685-700. 2003
    ..These compounds are therefore up to 18-fold more potent than EMATE, the very first highly potent irreversible steroidal STS inhibitor...
  24. ncbi request reprint Estrone 3-sulfate mimics, inhibitors of estrone sulfatase activity: homology model construction and docking studies
    Nicola M Howarth
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, UK
    Biochemistry 41:14801-14. 2002
    ..Docking studies using the substrate and estrone-3-sulfate mimics that are active inhibitors indicate they are positioned in the area of proposed catalysis, confirming the predictive power of the model...
  25. ncbi request reprint Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II
    Nigel Vicker
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem Lett 13:863-5. 2003
    ..The docking scores are compared with the inhibition of hCA II and show good correlation with biological activity...
  26. ncbi request reprint First dual aromatase-steroid sulfatase inhibitors
    L W Lawrence Woo
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, UK
    J Med Chem 46:3193-6. 2003
    ..82-100 nM (cf. letrozole, 0.89 nM). One dual inhibitor was potent against both enzymes in vivo, validating the concept...
  27. doi request reprint Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity
    Paul M Wood
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, UK
    J Med Chem 51:4226-38. 2008
    ..These results suggest that a new structural class of DASI for potential treatment of hormone-dependent breast cancer has been identified, and this is the first report of STS inhibition by an enantiopure nonsteroidal compound...
  28. ncbi request reprint Novel D-ring modified steroid derivatives as potent, non-estrogenic, steroid sulfatase inhibitors with in vivo activity
    Delphine S Fischer
    Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, UK
    J Steroid Biochem Mol Biol 84:343-9. 2003
    ..They were also devoid of estrogenic activity in the uterine weight gain assay, indicating that these two leads have therapeutic potential for the treatment of hormone-dependent breast cancer...
  29. ncbi request reprint Synthesis of D- and L-myo-inositol 1,2,4,6-tetrakisphosphate, regioisomers of myo-inositol 1,3,4,5 tetrakisphosphate: activity against Ins(1,4,5)P3 binding proteins
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, UK BA2 7AY
    Org Biomol Chem 1:3546-56. 2003
    ..The enantiomers of the 1,2,4,5-tetrakisphosphate showed the same relative pattern of activity towards the two enzymes but were more potent against 5-phosphatase (0.47 microM and 3 microM respectively)...
  30. doi request reprint Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents
    Mathew P Leese
    Department of Pharmacy and Pharmacology, University of Bath, Bath, UK
    J Med Chem 51:1295-308. 2008
    ..The potential of these multimechanism anticancer agents was confirmed in vivo, with promising activity observed for both 14 and 15 in an athymic nude mouse MDA-MB-231 human breast cancer xenograft model...
  31. ncbi request reprint Identification of mammalian Vps24p as an effector of phosphatidylinositol 3,5-bisphosphate-dependent endosome compartmentalization
    Paul Whitley
    Department of Biology and Biochemistry, University of Bath, United Kingdom
    J Biol Chem 278:38786-95. 2003
    ....
  32. doi request reprint Chimeric microtubule disruptors
    Mathew P Leese
    Medicinal Chemistry and Sterix Ltd, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Chem Commun (Camb) 46:2907-9. 2010
    ..Dosing of a representative chimera in a tumour xenograft model confirms the excellent therapeutic potential of the class...
  33. ncbi request reprint Aplysia californica mediated cyclisation of novel 3'-modified NAD+ analogues: a role for hydrogen bonding in the recognition of cyclic adenosine 5'-diphosphate ribose
    Christopher J W Mort
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Bioorg Med Chem 12:475-87. 2004
    ..5+/-0.5 microM. This high value suggests that the ability of the C3' substituent to donate a hydrogen bond is crucial for agonism...
  34. doi request reprint Structures of human carbonic anhydrase II/inhibitor complexes reveal a second binding site for steroidal and nonsteroidal inhibitors
    Gyles E Cozier
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    Biochemistry 49:3464-76. 2010
    ....
  35. ncbi request reprint First crystal structures of human carbonic anhydrase II in complex with dual aromatase-steroid sulfatase inhibitors
    Matthew D Lloyd
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    Biochemistry 44:6858-66. 2005
    ..Moreover, these results underpin the idea that binding to erythrocyte CA II may be a general method of stabilizing and delivering sulfamate-based drugs in vivo...
  36. ncbi request reprint Dual aromatase-sulfatase inhibitors based on the anastrozole template: synthesis, in vitro SAR, molecular modelling and in vivo activity
    Toby Jackson
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Org Biomol Chem 5:2940-52. 2007
    ..However, in vivo, 11 surprisingly exhibited potent dual inhibition. Compound 11 was modelled into the active site of a homology model of human aromatase and the X-ray crystal structure of steroid sulfatase...
  37. ncbi request reprint Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors
    Harshani R Lawrence
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, BA2 7AY, U K
    J Med Chem 48:2759-62. 2005
    ..A mode of binding is proposed for these inhibitors, and 2 is a steroid-based 17beta-HSD1 inhibitor with the potential for further development...
  38. pmc Crystal structure of human carbonic anhydrase II at 1.95 A resolution in complex with 667-coumate, a novel anti-cancer agent
    Matthew D Lloyd
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Biochem J 385:715-20. 2005
    ....
  39. ncbi request reprint Chemical synthesis of the second messenger nicotinic acid adenine dinucleotide phosphate by total synthesis of nicotinamide adenine dinucleotide phosphate
    James Dowden
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Angew Chem Int Ed Engl 43:4637-40. 2004
  40. doi request reprint Synthesis of aromatase inhibitors and dual aromatase steroid 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
    Christian Bubert
    Department of Pharmacy and Pharmacology and Sterix Ltd University of Bath, Claverton Down, Bath, UK
    ChemMedChem 3:1708-30. 2008
    ..These results further strengthen the concept of designing and developing DASIs for potential treatment of hormone-related cancers...
  41. doi request reprint 2'-deoxy cyclic adenosine 5'-diphosphate ribose derivatives: importance of the 2'-hydroxyl motif for the antagonistic activity of 8-substituted cADPR derivatives
    Bo Zhang
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, UK
    J Med Chem 51:1623-36. 2008
    ..The 2'-OH group, without effect on the Ca (2+)-mobilizing ability of cADPR itself, is an important motif for the antagonistic activities of 8-substituted cADPR analogues...
  42. ncbi request reprint 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)P(3) affinity matrix
    Andrew M Riley
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    Biochem Biophys Res Commun 318:444-52. 2004
    ..Thus, 5 is a new reactive Ins(1,4,5)P(3) analogue of considerable potential for investigation of the chemical biology of Ins(1,4,5)P(3)-mediated cellular signalling...
  43. ncbi request reprint Synthesis of potent Ins(1,4,5)P3 5-phosphatase inhibitors by modification of myo-inositol 1,3,4,6-tetrakisphosphate
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, BA2 7AY, Bath, UK
    Bioorg Med Chem 11:4245-53. 2003
    ..Thus, we have synthesised potent enzyme inhibitors, which do not mobilise Ca(2+) and devised conditions for quick, clean and inexpensive sulfoxidation of inositol polyphosphite intermediates...
  44. ncbi request reprint 3,17-disubstituted 2-alkylestra-1,3,5(10)-trien-3-ol derivatives: synthesis, in vitro and in vivo anticancer activity
    Christian Bubert
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    J Med Chem 50:4431-43. 2007
    ..3-O-Sulfamoylated 2-alkylestradiol-17-O-carbamates and sulfamates have considerable potential as anticancer agents...
  45. ncbi request reprint Dual aromatase-sulfatase inhibitors based on the anastrozole template: synthesis, in vitro SAR, molecular modelling and in vivo activity
    Toby Jackson
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Org Biomol Chem 5:2940-52. 2007
    ..However, in vivo, 11 surprisingly exhibited potent dual inhibition. Compound 11 was modelled into the active site of a homology model of human aromatase and the X-ray crystal structure of steroid sulfatase...
  46. doi request reprint Chemoenzymatic synthesis of 7-deaza cyclic adenosine 5'-diphosphate ribose analogues, membrane-permeant modulators of intracellular calcium release
    Bo Zhang
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom
    J Org Chem 73:1693-703. 2008
    ..3 was also found to be stable to enzyme-mediated hydrolysis using CD38 ectoenzyme...
  47. pmc Benzene polyphosphates as tools for cell signalling: inhibition of inositol 1,4,5-trisphosphate 5-phosphatase and interaction with the PH domain of protein kinase Balpha
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA27AY, UK
    Chembiochem 9:1757-66. 2008
    ..These new molecular tools will be of potential use in structural and cell signalling studies...
  48. ncbi request reprint 2-difluoromethyloestrone 3-O-sulphamate, a highly potent steroid sulphatase inhibitor
    Julie E Reed
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Biochem Biophys Res Commun 317:169-75. 2004
    ..H interactions between the 2-difluoromethyl group of (6) and hydrogen bond donor residues lining the catalytic site of STS might also contribute to the high potency observed for (6)...
  49. ncbi request reprint 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-lymph
    Christelle Moreau
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom
    J Med Chem 49:5162-76. 2006
    ....
  50. doi request reprint Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design
    Gillian M Allan
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down BA2 7AY, UK
    Bioorg Med Chem 16:4438-56. 2008
    ..Of the templates investigated biphenyl ethanone was promising and led to inhibitors with IC(50) values in the low micromolar range...
  51. ncbi request reprint 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
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Chembiochem 7:1696-706. 2006
    ..The effect of the phenolic 3-OH group in compound 4 confirms a critical role for the 6-OH group of the natural messenger in the dephosphorylation mechanism that persists even in radically modified analogues...
  52. ncbi request reprint Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
    Nigel Vicker
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, and St Mary s Hospital, London, UK
    ChemMedChem 1:464-81. 2006
    ..A new efficient diastereoselective synthesis of 25 has also been developed to facilitate supply for in vivo evaluation, and an X-ray crystal structure of this inhibitor is presented...
  53. ncbi request reprint Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase
    Hatem A M Hejaz
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem 12:2759-72. 2004
    ..BENZOMATE and related analogues therefore represent an important class of non-steroidal STS inhibitor and lead compounds for future drug design...
  54. ncbi request reprint Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, UK
    J Steroid Biochem Mol Biol 94:239-51. 2005
    ..The SAR parameters established herein will assist the future design of anti-proliferative and anti-endocrine agents as potential therapeutics for both hormone dependent and independent cancers...
  55. ncbi request reprint Dimers of D-myo-inositol 1,4,5-trisphosphate: design, synthesis, and interaction with Ins(1,4,5)P3 receptors
    Andrew M Riley
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Bioconjug Chem 15:278-89. 2004
    ..Possible interpretations of this result are considered in relation to the recently disclosed X-ray crystal structure of the type 1 Ins(1,4,5)P(3) receptor core binding domain...
  56. ncbi request reprint Rapid synthetic route toward structurally modified derivatives of cyclic adenosine 5'-diphosphate ribose
    Gerd K Wagner
    Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, United Kingdom
    J Org Chem 70:4810-9. 2005
    ..In Jurkat T-lymphocytes, N1-cIDPR 4 induced Ca2+ release with an almost identical profile as the natural agonist cADPR, illustrating the value of this approach...
  57. ncbi request reprint Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
    Nigel Vicker
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    J Steroid Biochem Mol Biol 104:123-9. 2007
    ..Docking studies with 1-3 into the crystal structure of human 11beta-HSD1 reveal how the molecules may interact with the enzyme and cofactor and give further scope for structure based drug design in the optimisation of these series...
  58. ncbi request reprint Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Mol Cell Endocrinol 248:214-7. 2006
    ..Docking studies with the benzothiazole derivative 1 into the crystal structure of human 11beta-HSD1 revealed how the molecule may interact with the enzyme and cofactor...
  59. ncbi request reprint Novel, potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
    Gillian M Allan
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down BA2 7AY, UK
    Mol Cell Endocrinol 248:204-7. 2006
    ..This work has shown that extension from this position on the pyrazole template is well tolerated and the optimization of such systems is under investigation...
  60. ncbi request reprint A definitive synthesis of D-myo-inositol 1,4,5,6-tetrakisphosphate and its enantiomer D-myo-inositol 3,4,5,6-tetrakisphosphate from a novel butane-2,3-diacetal-protected inositol
    Stephen J Mills
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK
    Chemistry 9:6207-14. 2003
    ..Biological activity of synthetic 1 b was confirmed in comparison with the natural polyphosphate...
  61. ncbi request reprint Synthesis and Ca2+-mobilizing activity of purine-modified mimics of adenophostin A: a model for the adenophostin-Ins(1,4,5)P3 receptor interaction
    Heidi J Rosenberg
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    J Med Chem 46:4860-71. 2003
    ..The docking results also point to specific interactions involving residues within the binding domain of the Ins(1,4,5)P(3) receptor that may be involved in the molecular recognition of the adenophostins...
  62. ncbi request reprint Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
    Gillian M Allan
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, BA2 7AY, UK
    J Med Chem 49:1325-45. 2006
    ..These amides are also selective for 17beta-HSD1 over 17beta-HSD2...
  63. ncbi request reprint The design of novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors
    Nigel Vicker
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Mol Cell Endocrinol 301:259-65. 2009
    ..Using our homology model as a tool for inhibitor design compound 5 was discovered as a novel potent and selective inhibitor of 17beta-HSD3 with an IC(50) approximately 200nM...
  64. ncbi request reprint Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Mol Cell Endocrinol 301:169-73. 2009
    ..Docking studies with the potent compound 8 into the crystal structure of human 11beta-HSD1 (1XU9) reveals how the molecule may interact with the enzyme and cofactor...
  65. ncbi request reprint Synthesis of glucopyranoside-based ligands for D-myo-inositol 1,4,5-trisphosphate receptors
    Andrew M Riley
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, UK
    Carbohydr Res 337:1067-82. 2002
    ..The route to furanophostin was further modified to give (3'S,4'R)-3'-hydroxytetrahydrofuran-4'-yl alpha-D-glucopyranoside 3'-phosphate 3,4-bisphosphorothioate, the first phosphorothioate-containing adenophostin analogue...
  66. ncbi request reprint A novel 18 beta-glycyrrhetinic acid analogue as a potent and selective inhibitor of 11 beta-hydroxysteroid dehydrogenase 2
    Nigel Vicker
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem Lett 14:3263-7. 2004
    ....
  67. doi request reprint Non-steroidal aromatase inhibitors based on a biphenyl scaffold: synthesis, in vitro SAR, and molecular modelling
    Toby Jackson
    Medicinal Chemistry, Department of Pharmacy and Pharmacology, and Sterix Ltd University of Bath, Claverton Down, UK
    ChemMedChem 3:603-18. 2008
    ..Further development of these compounds as potential therapeutic agents for the treatment of hormone-dependent breast cancer is warranted given the high level of potency observed for this class of aromatase inhibitor in vitro...
  68. doi request reprint 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
    Fabrice Jourdan
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, UK BA2 7AY
    Org Biomol Chem 6:4108-19. 2008
    ....
  69. pmc scyllo-inositol pentakisphosphate as an analogue of myo-inositol 1,3,4,5,6-pentakisphosphate: chemical synthesis, physicochemistry and biological applications
    Andrew M Riley
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, UK
    Chembiochem 7:1114-22. 2006
    ..This finding both reinforces the value of scyllo-InsP(5) as a biological control and shows that the axial 2-OH group of Ins(1,3,4,5,6)P(5) plays a part in substrate recognition by PTEN and the Ins(1,3,4,5,6)P(5) 2-kinases...
  70. ncbi request reprint Nicotinamide 2-fluoroadenine dinucleotide unmasks the NAD+ glycohydrolase activity of Aplysia californica adenosine 5'-diphosphate ribosyl cyclase
    Bo Zhang
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, United Kingdom
    Biochemistry 46:4100-9. 2007
    ..2-Fluoro-NAD+ is therefore a useful molecular tool allowing dissection of the kinetic scheme for this enzyme...
  71. doi request reprint Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors
    Xiangdong Su
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    ChemMedChem 5:1026-44. 2010
    ..Comparison of the publicly available X-ray crystal structures of human 11beta-HSD1 led to docking studies of the potent compounds, revealing how these molecules may interact with the enzyme and cofactor...
  72. ncbi request reprint On the contribution of stereochemistry to human ITPK1 specificity: Ins(1,4,5,6)P4 is not a physiologic substrate
    Andrew M Riley
    Wolfson Laboratory for Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    FEBS Lett 580:324-30. 2006
    ..18 microM) by inositolphosphate-multikinase...
  73. doi request reprint Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17-O,O-bis-sulfamate
    Fabrice Jourdan
    Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath BA2 7AY, U K
    J Med Chem 53:2942-51. 2010
    ..In addition, the SAR of 2-substituted estradiol-3-O-sulfamate derivatives as inhibitors of tubulin polymerization has been established for the first time. These agents inhibit the binding of radiolabeled colchicine to tubulin...
  74. ncbi request reprint A letrozole-based dual aromatase-sulphatase inhibitor with in vivo activity
    Paul M Wood
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down, Bath, England BA2 7AY, UK
    J Steroid Biochem Mol Biol 94:123-30. 2005
    ..Thus, the concept of a letrozole-based DASI has been validated and could be further developed and modified for therapeutic exploitation...
  75. ncbi request reprint 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
    Graeme Horne
    Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    Biochem Biophys Res Commun 320:1262-70. 2004
    ..We conclude that the 6-OH group in Ins(1,3,4,5)P(4) is crucial for its physicochemical behaviour and biological properties of this key inositol phosphate...
  76. ncbi request reprint E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1
    Delphine S Fischer
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Claverton Down BA2 7AY, U K
    J Med Chem 48:5749-70. 2005
    ..Molecular modeling studies, which support these findings, and a QSAR, the predictive power of which was demonstrated, are also presented...
  77. ncbi request reprint 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents
    Mathew P Leese
    Medicinal Chemistry, Department of Pharmacy and Pharmacology and Sterix Ltd, University of Bath, Bath BA2 7AY, UK
    Bioorg Med Chem Lett 14:3135-8. 2004
    ....
  78. ncbi request reprint Convergent synthesis and unexpected Ca(2+)-mobilizing activity of 8-substituted analogues of cyclic ADP-carbocyclic-ribose, a stable mimic of the Ca(2+)-mobilizing second messenger cyclic ADP-ribose
    Satoshi Shuto
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita 12, Nishi 6, Kita ku, Sapporo 060 0812, Japan
    J Med Chem 46:4741-9. 2003
    ..80 and 2 times less potent than cADPR, respectively. These data contribute to developing structure-activity relationships for the interaction of cADPR with its receptor...
  79. pmc The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer
    Paul A Foster
    Endocrinology and Metabolic Medicine, Faculty of Medicine, Imperial College London, St Mary s Hospital, London W2 1NY, United Kingdom
    Endocrinology 149:4035-42. 2008
    ..This novel study demonstrates for the first time that STS inhibitors are potent inhibitors of endometrial cancer growth in nude mice...
  80. ncbi request reprint Rapid functional assays of recombinant IP3 receptors
    Alex J Laude
    Department of Pharmacology, Tennis Court Road, Cambridge CB2 1PD, UK
    Cell Calcium 38:45-51. 2005
    ..The method allows quick and economical functional assays of recombinant IP3R in small volumes (< or = 100 microl)...
  81. ncbi request reprint Synthesis of stable and cell-type selective analogues of cyclic ADP-ribose, a Ca(2+)-mobilizing second messenger. Structure--activity relationship of the N1-ribose moiety
    Takashi Kudoh
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita 12, Nishi 6, Kita ku, Sapporo 060 0812, Japan
    J Am Chem Soc 127:8846-55. 2005
    ..Thus, this study represents an entry to cell-type selective cADPR analogues, which can be used as biological tools and/or novel drug leads...
  82. ncbi request reprint The role of steroid sulphatase in regulating the oestrogenicity of oestrogen sulphamates
    Surinder K Chander
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    Biochem Biophys Res Commun 322:217-22. 2004
    ..This enzyme therefore has a crucial role in regulating the oestrogenicity associated with this class of drug...
  83. ncbi request reprint Novel hydrolysis-resistant analogues of cyclic ADP-ribose: modification of the "northern" ribose and calcium release activity
    Andreas H Guse
    Institute for Medical Biochemistry and Molecular Biology, Division of Cellular Signal Transduction, University Hospital Hamburg Eppendorf, Martinistrasse 52, D 20246 Hamburg, Germany
    Biochemistry 41:6744-51. 2002
    ....
  84. ncbi request reprint Amplification and propagation of pacemaker Ca2+ signals by cyclic ADP-ribose and the type 3 ryanodine receptor in T cells
    Svenja Kunerth
    University Hospital Hamburg Eppendorf, Center for Experimental Medicine, Institute of Biochemistry and Molecular Biology I Cellular Signal Transduction, Martinistr 52, 20246 Hamburg, Germany
    J Cell Sci 117:2141-9. 2004
    ..Taken together, our results show that, under physiological conditions in human T cells, RyRs play crucial roles in the local amplification and the spatiotemporal development of subcellular Ca(2+) pacemaker signals...
  85. ncbi request reprint Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase
    Francesco Abbate
    Universita degli Studi di Firenze, Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Rm 188, I 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 14:231-4. 2004
    ..In addition, a very short bond of 1.78A between the zinc ion and the coordinated nitrogen atom of the sulfamate moiety is observed, which may explain the high affinity of this inhibitor for hCA II (K(i) of 10nM)...
  86. ncbi request reprint Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate
    Bindumalini Raobaikady
    Endocrinology and Metabolic Medicine, Faculty of Medicine and Sterix Ltd, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 84:351-8. 2003
    ..The anti-proliferative and STS inhibitory properties of 2-MeOE2bisMATE suggest that it has considerable potential for development as a novel anti-cancer drug...
  87. ncbi request reprint Development of a sensitive high-performance liquid chromatography method for the detection of 667 COUMATE in vivo
    Christopher R Ireson
    Endocrinology and Metabolic Medicine and Sterix Ltd, Faculty of Medicine, Imperial College, St Mary s Hospital, London W2 1NY, UK
    J Steroid Biochem Mol Biol 84:337-42. 2003
    ..In conclusion, the HPLC method developed is a reproducible and sensitive assay that will enable quantitation of the potent non-steroidal sulphatase inhibitor 667 COUMATE in biological fluids in the forthcoming Phase I clinical trial...
  88. ncbi request reprint Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor
    Susannah J Stanway
    Endocrinology and Metabolic Medicine and Sterix Ltd, UK
    Clin Cancer Res 12:1585-92. 2006
    ..Estrone and DHEA are formed by this sulfatase pathway and can be converted to steroids (estradiol and androstenediol, respectively), which have potent estrogenic properties...
  89. ncbi request reprint A systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Synthesis of beta-C-glucoside trisphosphates based on the conformational restriction strategy
    Masaru Terauchi
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita 12, Nishi 6, Kita ku, Sapporo 060 0812, Japan
    J Med Chem 49:1900-9. 2006
    ....
  90. ncbi request reprint Design and synthesis of 5'-deoxy-5'-phenyladenophostin A, a highly potent IP3 receptor ligand
    Tetsuya Mochizuki
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita 12, Nishi 6, Kita ku, Sapporo 060 0812, Japan
    Org Lett 8:1455-8. 2006
    ..This compound proved to be a highly potent IP(3) receptor agonist...
  91. doi request reprint 17beta-hydroxysteroid dehydrogenase Type 1, and not Type 12, is a target for endocrine therapy of hormone-dependent breast cancer
    Joanna M Day
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College London, St Mary s Hospital, London W2 1NY, United Kingdom
    Int J Cancer 122:1931-40. 2008
    ..Both E2 production and tumor growth were inhibited by STX1040, suggesting that 17beta-HSD1 inhibitors such as STX1040 may provide a novel treatment for hormone-dependent breast cancer...
  92. ncbi request reprint Efficacy of three potent steroid sulfatase inhibitors: pre-clinical investigations for their use in the treatment of hormone-dependent breast cancer
    Paul A Foster
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College Faculty of Medicine, St Mary s Hospital, London, W2 1NY, UK
    Breast Cancer Res Treat 111:129-38. 2008
    ..This study indicates that the STS inhibitor, STX213, exhibits excellent efficacy and pharmacokinetics and therefore offers a potentially novel treatment for hormone-dependent breast cancer...
  93. ncbi request reprint Interaction of the catalytic domain of inositol 1,4,5-trisphosphate 3-kinase A with inositol phosphate analogues
    Alexandra Poinas
    Interdisciplinary Research Institute IRIBHM, Universite Libre de Bruxelles, Campus Erasme, Bldg C, 808 Route de Lennik, 1070 Brussels, Belgium
    Chembiochem 6:1449-57. 2005
    ..Our data indicate the importance of the 3-hydroxy function in the mechanism of inositol trisphosphate phosphorylation rather than in substrate binding...
  94. ncbi request reprint Catalysis-associated conformational changes revealed by human CD38 complexed with a non-hydrolyzable substrate analog
    Qun Liu
    MacCHESS, Cornell High Energy Synchrotron Source, Cornell University, Ithaca, New York 14853, USA
    J Biol Chem 282:24825-32. 2007
    ..The binary CD38-cADPR model described here represents the most detailed description of the CD38-catalyzed hydrolysis of cADPR at atomic resolution. Our structural model should provide insights into the design of effective cADPR analogs...
  95. ncbi request reprint Novel inositol phospholipid headgroup surrogate crystallized in the pleckstrin homology domain of protein kinase Balpha
    Stephen J Mills
    ACS Chem Biol 2:242-6. 2007
    ..Bz(1,2,3,4)P4 is an example of a simple inositol phosphate surrogate crystallized in a protein, and this approach could be applied to design modulators of inositol polyphosphate binding proteins...
  96. ncbi request reprint In vivo efficacy of STX213, a second-generation steroid sulfatase inhibitor, for hormone-dependent breast cancer therapy
    Paul A Foster
    Department of Endocrinology and Metabolic Medicine and Sterix Ltd, Imperial College Faculty of Medicine, St Mary s Hospital, London, United Kingdom
    Clin Cancer Res 12:5543-9. 2006
    ..We compare the in vivo efficacy of two potent STS inhibitors, STX64 and STX213, in a xenograft breast cancer model...
  97. ncbi request reprint Synthesis of adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP3 receptor ligands
    Tetsuya Mochizuki
    Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo 060 0812, Japan
    J Med Chem 49:5750-8. 2006
    ..This biological activity of 5a-c can be rationalized by molecular modeling using the ligand binding domain of the IP(3) receptor...
  98. ncbi request reprint Cell-permeant small-molecule modulators of NAADP-mediated Ca2+ release
    James Dowden
    School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, United Kingdom
    Chem Biol 13:659-65. 2006
    ....
  99. pmc Determinants of adenophostin A binding to inositol trisphosphate receptors
    Stephen A Morris
    Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD, U K
    Biochem J 367:113-20. 2002
    ..In addition we suggest that C-terminal residues, which impede access of IP(3), may selectively interact with adenophostin A to allow it unhindered access to the IP(3)-binding domain...