Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target

Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target

Inhibition of the Trypanosoma cruzi cysteine protease cruzain has been proposed as a therapeutic approach for the treatment of Chagas’ disease. Among the best-studied cruzain inhibitors to date is the vinylsulfone K777 (1), which has proven effective in animal models of Chagas’ disease. Recent struc...

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Bibliographic Details
Main Authors: Jonathan W. Choy, Clifford Bryant, Claudia M. Calvet, Patricia S. Doyle, Shamila S. Gunatilleke, Siegfried S. F. Leung, Kenny K. H. Ang, Steven Chen, Jiri Gut, Juan A. Oses-Prieto, Jonathan B. Johnston, Michelle R. Arkin, Alma L. Burlingame, Jack Taunton, Matthew P. Jacobson, James M. McKerrow, Larissa M. Podust, Adam R. Renslo
Format: Article
Language:English
Published: Beilstein-Institut 2013-01-01
Series:Beilstein Journal of Organic Chemistry
Subjects:
activity-based probes
Chagas’ disease
cruzain
CYP51
14-α-demethylase
hybrid drugs
Trypanosoma cruzi
Online Access:https://doi.org/10.3762/bjoc.9.3

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