Structure-guided development of selective TbcatB inhibitors

Jeremy P. Mallari, Anang A. Shelat, Aaron Kosinski, Conor R. Caffrey, Michele Connelly, Fangyi Zhu, James H. McKerrow, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

23 Scopus citations


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.

Original languageEnglish
Pages (from-to)6489-6493
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number20
StatePublished - Oct 22 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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