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596 results

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Page 1
Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function.
Saalau-Bethell SM, Woodhead AJ, Chessari G, Carr MG, Coyle J, Graham B, Hiscock SD, Murray CW, Pathuri P, Rich SJ, Richardson CJ, Williams PA, Jhoti H. Saalau-Bethell SM, et al. Among authors: williams pa. Nat Chem Biol. 2012 Nov;8(11):920-5. doi: 10.1038/nchembio.1081. Epub 2012 Sep 30. Nat Chem Biol. 2012. PMID: 23023261 Free PMC article.
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
Chessari G, Buck IM, Day JE, Day PJ, Iqbal A, Johnson CN, Lewis EJ, Martins V, Miller D, Reader M, Rees DC, Rich SJ, Tamanini E, Vitorino M, Ward GA, Williams PA, Williams G, Wilsher NE, Woolford AJ. Chessari G, et al. Among authors: williams pa, williams g. J Med Chem. 2015 Aug 27;58(16):6574-88. doi: 10.1021/acs.jmedchem.5b00706. Epub 2015 Aug 7. J Med Chem. 2015. PMID: 26218264
Fragment-based drug discovery using cryo-EM.
Saur M, Hartshorn MJ, Dong J, Reeks J, Bunkoczi G, Jhoti H, Williams PA. Saur M, et al. Among authors: williams pa. Drug Discov Today. 2020 Mar;25(3):485-490. doi: 10.1016/j.drudis.2019.12.006. Epub 2019 Dec 23. Drug Discov Today. 2020. PMID: 31877353 Free article. Review.
Cryo-EM in drug discovery.
Ceska T, Chung CW, Cooke R, Phillips C, Williams PA. Ceska T, et al. Among authors: williams pa. Biochem Soc Trans. 2019 Feb 28;47(1):281-293. doi: 10.1042/BST20180267. Epub 2019 Jan 15. Biochem Soc Trans. 2019. PMID: 30647139 Review.
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Tamanini E, Buck IM, Chessari G, Chiarparin E, Day JEH, Frederickson M, Griffiths-Jones CM, Hearn K, Heightman TD, Iqbal A, Johnson CN, Lewis EJ, Martins V, Peakman T, Reader M, Rich SJ, Ward GA, Williams PA, Wilsher NE. Tamanini E, et al. Among authors: williams pa. J Med Chem. 2017 Jun 8;60(11):4611-4625. doi: 10.1021/acs.jmedchem.6b01877. Epub 2017 May 24. J Med Chem. 2017. PMID: 28492317
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G. Johnson CN, et al. Among authors: williams pa. J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9. J Med Chem. 2018. PMID: 30091600
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
Howard S, Amin N, Benowitz AB, Chiarparin E, Cui H, Deng X, Heightman TD, Holmes DJ, Hopkins A, Huang J, Jin Q, Kreatsoulas C, Martin AC, Massey F, McCloskey L, Mortenson PN, Pathuri P, Tisi D, Williams PA. Howard S, et al. Among authors: williams pa. ACS Med Chem Lett. 2013 Oct 18;4(12):1208-12. doi: 10.1021/ml4003277. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900632 Free PMC article.
596 results