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In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR Jr, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE. Costanzo MJ, et al. Among authors: kauffman ja. J Med Chem. 2005 Mar 24;48(6):1984-2008. doi: 10.1021/jm0303857. J Med Chem. 2005. PMID: 15771442
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.
Costanzo MJ, Yabut SC, Almond HR Jr, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D, Maryanoff BE. Costanzo MJ, et al. Among authors: kauffman ja. J Med Chem. 2003 Aug 28;46(18):3865-76. doi: 10.1021/jm030050p. J Med Chem. 2003. PMID: 12930148
A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ, Kauffman JA, Corcoran TW, Derian CK, Eckardt AJ, Damiano BP, Andrade-Gordon P, Maryanoff BE. de Garavilla L, et al. Among authors: kauffman ja. J Biol Chem. 2005 May 6;280(18):18001-7. doi: 10.1074/jbc.M501302200. Epub 2005 Feb 28. J Biol Chem. 2005. PMID: 15741158 Free article.
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC. Hoekstra WJ, et al. Among authors: kauffman ja. J Med Chem. 1999 Dec 16;42(25):5254-65. doi: 10.1021/jm990418b. J Med Chem. 1999. PMID: 10602710
32 results