Structure-Guided Development of Selective TbcatB Inhibitors

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, try...

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Veröffentlicht in:	Journal of medicinal chemistry 2009-10, Vol.52 (20), p.6489-6493
Hauptverfasser:	Mallari, Jeremy P, Shelat, Anang A, Kosinski, Aaron, Caffrey, Conor R, Connelly, Michele, Zhu, Fangyi, McKerrow, James H, Guy, R. Kiplin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Cathepsin B - antagonists & inhibitors Cathepsin B - metabolism Cathepsin L - antagonists & inhibitors Cathepsin L - metabolism Cell Line Cysteine Endopeptidases - chemistry Cysteine Endopeptidases - metabolism Drug Discovery Humans Medical sciences Models, Molecular Pharmacology. Drug treatments Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Protein Conformation Purines - chemistry Substrate Specificity Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma brucei brucei - drug effects Trypanosoma brucei brucei - enzymology
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