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.
|Number of pages||5|
|Journal||Journal of Medicinal Chemistry|
|State||Published - Oct 22 2009|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery