Document Report Card

ID: ALA1155239

Journal: J Med Chem

Title: Structure-guided development of selective TbcatB inhibitors.

Authors: Mallari JP, Shelat AA, Kosinski A, Caffrey CR, Connelly M, Zhu F, McKerrow JH, Guy RK.

Abstract: The trypanosomal cathepsin TbcatB is essential for parasite survival and is an attractive therapeutic target. Herein we report the structure-guided development of TbcatB inhibitors with specificity relative to rhodesain and human cathepsins B and L. Inhibitors were tested for enzymatic activity, trypanocidal activity, and general cytotoxicity. These data chemically validate TbcatB as a drug target and demonstrate that it is possible to potently and selectively inhibit TbcatB relative to trypanosomal and human homologues.

CiteXplore: 19769357

DOI: 10.1021/jm900908p