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Page 1
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: westaway sm. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
Structural analysis of human KDM5B guides histone demethylase inhibitor development.
Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U. Johansson C, et al. Nat Chem Biol. 2016 Jul;12(7):539-45. doi: 10.1038/nchembio.2087. Epub 2016 May 23. Nat Chem Biol. 2016. PMID: 27214403
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. J Med Chem. 2016 Feb 25;59(4):1357-69. doi: 10.1021/acs.jmedchem.5b01537. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771107
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. J Med Chem. 2016 Feb 25;59(4):1370-87. doi: 10.1021/acs.jmedchem.5b01538. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771203
Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S. Hatch SB, et al. Among authors: westaway sm. Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017. Epigenetics Chromatin. 2017. PMID: 28265301 Free PMC article.
Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics.
Joberty G, Boesche M, Brown JA, Eberhard D, Garton NS, Humphreys PG, Mathieson T, Muelbaier M, Ramsden NG, Reader V, Rueger A, Sheppard RJ, Westaway SM, Bantscheff M, Lee K, Wilson DM, Prinjha RK, Drewes G. Joberty G, et al. Among authors: westaway sm. ACS Chem Biol. 2016 Jul 15;11(7):2002-10. doi: 10.1021/acschembio.6b00080. Epub 2016 May 19. ACS Chem Biol. 2016. PMID: 27197014
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Bailey JM, Scott JS, Basilla JB, Bolton VJ, Boyfield I, Evans DG, Fleury E, Heightman TD, Jarvie EM, Lawless K, Matthews KL, McKay F, Mok H, Muir A, Orlek BS, Sanger GJ, Stemp G, Stevens AJ, Thompson M, Ward J, Vaidya K, Westaway SM. Bailey JM, et al. Among authors: westaway sm. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6452-8. doi: 10.1016/j.bmcl.2009.09.027. Epub 2009 Sep 12. Bioorg Med Chem Lett. 2009. PMID: 19804969
Tetrahydroquinoline derivatives as opioid receptor antagonists.
Zhang C, Westaway SM, Speake JD, Bishop MJ, Goetz AS, Carballo LH, Hu M, Epperly AH. Zhang C, et al. Among authors: westaway sm. Bioorg Med Chem Lett. 2011 Jan 15;21(2):670-6. doi: 10.1016/j.bmcl.2010.12.010. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21193310
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Westaway SM, Brown SL, Fell SC, Johnson CN, MacPherson DT, Mitchell DJ, Myatt JW, Stanway SJ, Seal JT, Stemp G, Thompson M, Lawless K, McKay F, Muir AI, Barford JM, Cluff C, Mahmood SR, Matthews KL, Mohamed S, Smith B, Stevens AJ, Bolton VJ, Jarvie EM, Sanger GJ. Westaway SM, et al. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. J Med Chem. 2009. PMID: 19191554
Identification of small molecule agonists of the motilin receptor.
Heightman TD, Conway E, Corbett DF, Macdonald GJ, Stemp G, Westaway SM, Celestini P, Gagliardi S, Riccaboni M, Ronzoni S, Vaidya K, Butler S, McKay F, Muir A, Powney B, Winborn K, Wise A, Jarvie EM, Sanger GJ. Heightman TD, et al. Among authors: westaway sm. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6423-8. doi: 10.1016/j.bmcl.2008.10.071. Epub 2008 Oct 19. Bioorg Med Chem Lett. 2008. PMID: 18980843
17 results