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American Chemical Society, Journal of Medicinal Chemistry, 20(52), p. 6489-6493, 2009

DOI: 10.1021/jm900908p

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Structure-guided development of selective TbcatB inhibitors

Journal article published in 2009 by Jeremy P. Mallari, Anang A. Shelat, Aaron Kosinski, Conor R. Caffrey, Michele Connelly, Fangyi Zhu, James H. McKerrow, R. Kiplin Guy ORCID
This paper is available in a repository.
This paper is available in a repository.

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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.