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Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.
Safina BS, Baker S, Baumgardner M, Blaney PM, Chan BK, Chen YH, Cartwright MW, Castanedo G, Chabot C, Cheguillaume AJ, Goldsmith P, Goldstein DM, Goyal B, Hancox T, Handa RK, Iyer PS, Kaur J, Kondru R, Kenny JR, Krintel SL, Li J, Lesnick J, Lucas MC, Lewis C, Mukadam S, Murray J, Nadin AJ, Nonomiya J, Padilla F, Palmer WS, Pang J, Pegg N, Price S, Reif K, Salphati L, Savy PA, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Tay S, Tivitmahaisoon P, Waszkowycz B, Wei B, Yue Q, Zhang C, Sutherlin DP. Safina BS, et al. Among authors: nadin aj. J Med Chem. 2012 Jun 28;55(12):5887-900. doi: 10.1021/jm3003747. Epub 2012 Jun 11. J Med Chem. 2012. PMID: 22626259
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B. Sutherlin DP, et al. Among authors: nadin aj. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672799
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity.
Barnes L, Blaber H, Brooks DTK, Byers L, Buckley D, Byron ZC, Chilvers RG, Cochrane L, Cooney E, Damian HA, Francis L, Fu He D, Grace JMJ, Green HJ, Hogarth EJP, Jusu L, Killalea CE, King O, Lambert J, Lee ZJ, Lima NS, Long CL, Mackinnon ML, Mahdy S, Matthews-Wright J, Millward MJ, Meehan MF, Merrett C, Morrison L, Parke HRI, Payne C, Payne L, Pike C, Seal A, Senior AJ, Smith KM, Stanelyte K, Stillibrand J, Szpara R, Taday FFH, Threadgould AM, Trainor RJ, Waters J, Williams O, Wong CKW, Wood K, Barton N, Gruszka A, Henley Z, Rowedder JE, Cookson R, Jones KL, Nadin A, Smith IE, Macdonald SJF, Nortcliffe A. Barnes L, et al. Among authors: nadin a. J Med Chem. 2019 Nov 27;62(22):10402-10422. doi: 10.1021/acs.jmedchem.9b01499. Epub 2019 Nov 6. J Med Chem. 2019. PMID: 31647659
3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.
Shaw D, Best J, Dinnell K, Nadin A, Shearman M, Pattison C, Peachey J, Reilly M, Williams B, Wrigley J, Harrison T. Shaw D, et al. Among authors: nadin a. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3073-7. doi: 10.1016/j.bmcl.2005.12.083. Epub 2006 Apr 17. Bioorg Med Chem Lett. 2006. PMID: 16617016
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