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J Med Chem. 2009 Oct 22;52(20):6489-93. doi: 10.1021/jm900908p.

Structure-guided development of selective TbcatB inhibitors.

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1
Graduate Program in Chemistry and Chemical Biology, University of California, San Francisco, California 94143-2280, USA.

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.

PMID:
19769357
PMCID:
PMC2762491
DOI:
10.1021/jm900908p
[Indexed for MEDLINE]
Free PMC Article
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