Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 20, Pages 6489-6493Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm900908p
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Funding
- American Lebanese Syrian Associated Charities (ALSAC)
- Children's Research Hospital, National Institute of Allergy and Infectious Diseases [AI35707]
- Drugs for Neglected Diseases initiative
- Sandler Family Supporting Foundation
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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.
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