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Page 1
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.
Patel L, Chandrasekhar J, Evarts J, Haran AC, Ip C, Kaplan JA, Kim M, Koditek D, Lad L, Lepist EI, McGrath ME, Novikov N, Perreault S, Puri KD, Somoza JR, Steiner BH, Stevens KL, Therrien J, Treiberg J, Villaseñor AG, Yeung A, Phillips G. Patel L, et al. Among authors: mcgrath me. J Med Chem. 2016 Apr 14;59(7):3532-48. doi: 10.1021/acs.jmedchem.6b00213. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26980109
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
Patel L, Chandrasekhar J, Evarts J, Forseth K, Haran AC, Ip C, Kashishian A, Kim M, Koditek D, Koppenol S, Lad L, Lepist EI, McGrath ME, Perreault S, Puri KD, Villaseñor AG, Somoza JR, Steiner BH, Therrien J, Treiberg J, Phillips G. Patel L, et al. Among authors: mcgrath me. J Med Chem. 2016 Oct 13;59(19):9228-9242. doi: 10.1021/acs.jmedchem.6b01169. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27660855
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G. Perreault S, et al. Among authors: mcgrath me. J Med Chem. 2017 Feb 23;60(4):1555-1567. doi: 10.1021/acs.jmedchem.6b01821. Epub 2017 Feb 7. J Med Chem. 2017. PMID: 28106991
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor.
Chandrasekhar J, Dick R, Van Veldhuizen J, Koditek D, Lepist EI, McGrath ME, Patel L, Phillips G, Sedillo K, Somoza JR, Therrien J, Till NA, Treiberg J, Villaseñor AG, Zherebina Y, Perreault S. Chandrasekhar J, et al. Among authors: mcgrath me. J Med Chem. 2018 Aug 9;61(15):6858-6868. doi: 10.1021/acs.jmedchem.8b00797. Epub 2018 Jul 30. J Med Chem. 2018. PMID: 30015489
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Perreault S, Arjmand F, Chandrasekhar J, Hao J, Keegan KS, Koditek D, Lepist EI, Matson CK, McGrath ME, Patel L, Sedillo K, Therrien J, Till NA, Tomkinson A, Treiberg J, Zherebina Y, Phillips G. Perreault S, et al. Among authors: mcgrath me. ACS Med Chem Lett. 2020 Apr 13;11(6):1236-1243. doi: 10.1021/acsmedchemlett.0c00095. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551006 Free PMC article.
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Palmer JT, Bryant C, Wang DX, Davis DE, Setti EL, Rydzewski RM, Venkatraman S, Tian ZQ, Burrill LC, Mendonca RV, Springman E, McCarter J, Chung T, Cheung H, Janc JW, McGrath M, Somoza JR, Enriquez P, Yu ZW, Strickley RM, Liu L, Venuti MC, Percival MD, Falgueyret JP, Prasit P, Oballa R, Riendeau D, Young RN, Wesolowski G, Rodan SB, Johnson C, Kimmel DB, Rodan G. Palmer JT, et al. J Med Chem. 2005 Dec 1;48(24):7520-34. doi: 10.1021/jm058198r. J Med Chem. 2005. PMID: 16302794
Peptide ketobenzoxazole inhibitors bound to cathepsin K.
McGrath ME, Sprengeler PA, Hill CM, Martichonok V, Cheung H, Somoza JR, Palmer JT, Janc JW. McGrath ME, et al. Biochemistry. 2003 Dec 30;42(51):15018-28. doi: 10.1021/bi035041x. Biochemistry. 2003. PMID: 14690410
Crystal structure of human cathepsin S.
McGrath ME, Palmer JT, Brömme D, Somoza JR. McGrath ME, et al. Protein Sci. 1998 Jun;7(6):1294-302. doi: 10.1002/pro.5560070604. Protein Sci. 1998. PMID: 9655332 Free PMC article.
110 results