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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. Among authors: mcgrath m. 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
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Sperandio D, Tai VW, Lohman J, Hirschbein B, Mendonca R, Lee CS, Spencer JR, Janc J, Nguyen M, Beltman J, Sprengeler P, Scheerens H, Lin T, Liu L, Gadre A, Kellogg A, Green MJ, McGrath ME. Sperandio D, et al. Among authors: mcgrath me. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24. Bioorg Med Chem Lett. 2006. PMID: 16725321
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.
Structure-guided design of peptide-based tryptase inhibitors.
McGrath ME, Sprengeler PA, Hirschbein B, Somoza JR, Lehoux I, Janc JW, Gjerstad E, Graupe M, Estiarte A, Venkataramani C, Liu Y, Yee R, Ho JD, Green MJ, Lee CS, Liu L, Tai V, Spencer J, Sperandio D, Katz BA. McGrath ME, et al. Biochemistry. 2006 May 16;45(19):5964-73. doi: 10.1021/bi060173m. Biochemistry. 2006. PMID: 16681368
Crystal structure of human cathepsin V.
Somoza JR, Zhan H, Bowman KK, Yu L, Mortara KD, Palmer JT, Clark JM, McGrath ME. Somoza JR, et al. Among authors: mcgrath me. Biochemistry. 2000 Oct 17;39(41):12543-51. doi: 10.1021/bi000951p. Biochemistry. 2000. PMID: 11027133
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
1,291 results