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Page 1
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.
Cho YS, Levell JR, Liu G, Caferro T, Sutton J, Shafer CM, Costales A, Manning JR, Zhao Q, Sendzik M, Shultz M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Kulathila R, Xie X, Dodd S, Gould T, Liang G, Heimbach T, Slocum K, Firestone B, Pu M, Pagliarini R, Growney JD. Cho YS, et al. Among authors: kulathila r. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. doi: 10.1021/acsmedchemlett.7b00342. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057061 Free PMC article.
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS. Levell JR, et al. Among authors: kulathila r. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. doi: 10.1021/acsmedchemlett.6b00334. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197303 Free PMC article.
Allosteric Mutant IDH1 Inhibitors Reveal Mechanisms for IDH1 Mutant and Isoform Selectivity.
Xie X, Baird D, Bowen K, Capka V, Chen J, Chenail G, Cho Y, Dooley J, Farsidjani A, Fortin P, Kohls D, Kulathila R, Lin F, McKay D, Rodrigues L, Sage D, Touré BB, van der Plas S, Wright K, Xu M, Yin H, Levell J, Pagliarini RA. Xie X, et al. Among authors: kulathila r. Structure. 2017 Mar 7;25(3):506-513. doi: 10.1016/j.str.2016.12.017. Epub 2017 Jan 26. Structure. 2017. PMID: 28132785 Free article.
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z. Papillon JPN, et al. Among authors: kulathila r. J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339381
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13.
Tommasi RA, Weiler S, McQuire LW, Rogel O, Chambers M, Clark K, Doughty J, Fang J, Ganu V, Grob J, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Melton R, Springer C, Walker M, Zhang J, Zhu L, Shultz M. Tommasi RA, et al. Among authors: kulathila r. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6440-5. doi: 10.1016/j.bmcl.2011.08.087. Epub 2011 Aug 27. Bioorg Med Chem Lett. 2011. PMID: 21937229
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Touré BB, Miller-Moslin K, Yusuff N, Perez L, Doré M, Joud C, Michael W, DiPietro L, van der Plas S, McEwan M, Lenoir F, Hoe M, Karki R, Springer C, Sullivan J, Levine K, Fiorilla C, Xie X, Kulathila R, Herlihy K, Porter D, Visser M. Touré BB, et al. Among authors: kulathila r. ACS Med Chem Lett. 2013 Jan 4;4(2):186-90. doi: 10.1021/ml300321d. eCollection 2013 Feb 14. ACS Med Chem Lett. 2013. PMID: 24900652 Free PMC article.
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
Monovich LG, Tommasi RA, Fujimoto RA, Blancuzzi V, Clark K, Cornell WD, Doti R, Doughty J, Fang J, Farley D, Fitt J, Ganu V, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Parker DT, Melton R, O'Byrne E, Pastor G, Pellas T, Quadros E, Reel N, Roland DM, Sakane Y, Singh H, Skiles J, Somers J, Toscano K, Wigg A, Zhou S, Zhu L, Shieh WC, Xue S, McQuire LW. Monovich LG, et al. Among authors: kulathila r. J Med Chem. 2009 Jun 11;52(11):3523-38. doi: 10.1021/jm801394m. J Med Chem. 2009. PMID: 19422229
23 results