3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)

…, J Morser, L Zhao, R Vergona, K White, M Adler…

Index: Islam, Imadul; Bryant, Judi; May, Karen; Mohan, Raju; Yuan, Shendong; Kent, Lorraine; Morser, John; Zhao, Lei; Vergona, Ron; White, Kathy; Adler, Marc; Whitlow, Marc; Buckman, Brad O. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1349 - 1354

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Citation Number: 19

Abstract

A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B.(−) 2a ...