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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK. Seal J, et al. Among authors: prinjha rk. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24. Bioorg Med Chem Lett. 2012. PMID: 22437115
Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors.
Bandukwala HS, Gagnon J, Togher S, Greenbaum JA, Lamperti ED, Parr NJ, Molesworth AM, Smithers N, Lee K, Witherington J, Tough DF, Prinjha RK, Peters B, Rao A. Bandukwala HS, et al. Among authors: prinjha rk. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7. doi: 10.1073/pnas.1212264109. Epub 2012 Aug 21. Proc Natl Acad Sci U S A. 2012. PMID: 22912406 Free PMC article.
BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms.
Wyspiańska BS, Bannister AJ, Barbieri I, Nangalia J, Godfrey A, Calero-Nieto FJ, Robson S, Rioja I, Li J, Wiese M, Cannizzaro E, Dawson MA, Huntly B, Prinjha RK, Green AR, Gottgens B, Kouzarides T. Wyspiańska BS, et al. Among authors: prinjha rk. Leukemia. 2014 Jan;28(1):88-97. doi: 10.1038/leu.2013.234. Epub 2013 Aug 9. Leukemia. 2014. PMID: 23929215
Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.
Chaidos A, Caputo V, Gouvedenou K, Liu B, Marigo I, Chaudhry MS, Rotolo A, Tough DF, Smithers NN, Bassil AK, Chapman TD, Harker NR, Barbash O, Tummino P, Al-Mahdi N, Haynes AC, Cutler L, Le B, Rahemtulla A, Roberts I, Kleijnen M, Witherington JJ, Parr NJ, Prinjha RK, Karadimitris A. Chaidos A, et al. Among authors: prinjha rk. Blood. 2014 Jan 30;123(5):697-705. doi: 10.1182/blood-2013-01-478420. Epub 2013 Dec 13. Blood. 2014. PMID: 24335499 Free article.
153 results