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Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2).
Day JEH, Berdini V, Castro J, Chessari G, Davies TG, Day PJ, St Denis JD, Fujiwara H, Fukaya S, Hamlett CCF, Hearn K, Hiscock SD, Holvey RS, Ito S, Kandola N, Kodama Y, Liebeschuetz JW, Martins V, Matsuo K, Mortenson PN, Muench S, Nakatsuru Y, Ochiiwa H, Palmer N, Peakman T, Price A, Reader M, Rees DC, Rich SJ, Shah A, Shibata Y, Smyth T, Twigg DG, Wallis NG, Williams G, Wilsher NE, Woodhead A, Shimamura T, Johnson CN. Day JEH, et al. J Med Chem. 2024 Mar 28;67(6):4655-4675. doi: 10.1021/acs.jmedchem.3c02118. Epub 2024 Mar 10. J Med Chem. 2024. PMID: 38462716
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.
Murray CW, Berdini V, Buck IM, Carr ME, Cleasby A, Coyle JE, Curry JE, Day JE, Day PJ, Hearn K, Iqbal A, Lee LY, Martins V, Mortenson PN, Munck JM, Page LW, Patel S, Roomans S, Smith K, Tamanini E, Saxty G. Murray CW, et al. ACS Med Chem Lett. 2015 Jun 4;6(7):798-803. doi: 10.1021/acsmedchemlett.5b00143. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191369 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. 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
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: day jeh. 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
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Heightman TD, et al. Among authors: day jeh. J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31. J Med Chem. 2018. PMID: 29775310
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: day jeh. 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
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Bevan L, Buck IM, Carr MG, Courtin A, Coyle JE, Day JEH, East C, Fazal L, Griffiths-Jones CM, Howard S, Kucia-Tran J, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Peakman TM, Reader M, Rees DC, Rich SJ, Shah A, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Heightman TD, et al. Among authors: day jeh. J Med Chem. 2021 Aug 26;64(16):12286-12303. doi: 10.1021/acs.jmedchem.1c00905. Epub 2021 Aug 13. J Med Chem. 2021. PMID: 34387469
12 results