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Page 1
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation.
Winter JJ, Anderson M, Blades K, Brassington C, Breeze AL, Chresta C, Embrey K, Fairley G, Faulder P, Finlay MR, Kettle JG, Nowak T, Overman R, Patel SJ, Perkins P, Spadola L, Tart J, Tucker JA, Wrigley G. Winter JJ, et al. Among authors: tart j. J Med Chem. 2015 Mar 12;58(5):2265-74. doi: 10.1021/jm501660t. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25695162 Free article.
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Ward RA, Brassington C, Breeze AL, Caputo A, Critchlow S, Davies G, Goodwin L, Hassall G, Greenwood R, Holdgate GA, Mrosek M, Norman RA, Pearson S, Tart J, Tucker JA, Vogtherr M, Whittaker D, Wingfield J, Winter J, Hudson K. Ward RA, et al. Among authors: tart j. J Med Chem. 2012 Apr 12;55(7):3285-306. doi: 10.1021/jm201734r. Epub 2012 Mar 26. J Med Chem. 2012. PMID: 22417091
Rapid Identification of Novel Allosteric PRC2 Inhibitors.
Read JA, Tart J, Rawlins PB, Gregson C, Jones K, Gao N, Zhu X, Tomlinson R, Code E, Cheung T, Chen H, Kawatkar SP, Bloecher A, Bagal S, O'Donovan DH, Robinson J. Read JA, et al. Among authors: tart j. ACS Chem Biol. 2019 Oct 18;14(10):2134-2140. doi: 10.1021/acschembio.9b00468. Epub 2019 Sep 23. ACS Chem Biol. 2019. PMID: 31525019
Identification and Characterization of Dual Inhibitors of the USP25/28 Deubiquitinating Enzyme Subfamily.
Wrigley JD, Gavory G, Simpson I, Preston M, Plant H, Bradley J, Goeppert AU, Rozycka E, Davies G, Walsh J, Valentine A, McClelland K, Odrzywol KE, Renshaw J, Boros J, Tart J, Leach L, Nowak T, Ward RA, Harrison T, Andrews DM. Wrigley JD, et al. Among authors: tart j. ACS Chem Biol. 2017 Dec 15;12(12):3113-3125. doi: 10.1021/acschembio.7b00334. Epub 2017 Nov 28. ACS Chem Biol. 2017. PMID: 29131570
High throughput application of the NanoBiT Biochemical Assay for the discovery of selective inhibitors of the interaction of PI3K-p110α with KRAS.
Ismail M, Davies G, Sproat G, Monteverde T, Tart J, Acebrón-García-de-Eulate M, Gohlke A, Hancock D, Adhikari S, Stefanovic-Barrett S, Smith DM, Flemington V, Gleave-Hanford ES, Holdgate GA, Kettle JG, Downward J. Ismail M, et al. Among authors: tart j. SLAS Discov. 2024 Dec;29(8):100197. doi: 10.1016/j.slasd.2024.100197. Epub 2024 Nov 28. SLAS Discov. 2024. PMID: 39613028 Free article.
Fragment-Based Discovery of Novel MUS81 Inhibitors.
Collie GW, Börjesson U, Chen Y, Dong Z, Di Fruscia P, Gohlke A, Hoyle A, Hunt TA, Jesani MH, Luo H, Luptak J, Milbradt AG, Narasimhan P, Packer M, Patel S, Qiao J, Storer RI, Stubbs CJ, Tart J, Truman C, Wang AT, Wheeler MG, Winter-Holt J. Collie GW, et al. Among authors: tart j. ACS Med Chem Lett. 2024 Jun 7;15(7):1151-1158. doi: 10.1021/acsmedchemlett.3c00453. eCollection 2024 Jul 11. ACS Med Chem Lett. 2024. PMID: 39015284 Free PMC article.
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