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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Autors principals: Choy, Jonathan W, Bryant, Clifford, Calvet, Claudia M, Doyle, Patricia S, Gunatilleke, Shamila S, Leung, Siegfried S F, Ang, Kenny K H, Chen, Steven, Gut, Jiri, Oses-Prieto, Juan A, Johnston, Jonathan B, Arkin, Michelle R, Burlingame, Alma L, Taunton, Jack, Jacobson, Matthew P, McKerrow, James M, Podust, Larissa M, Renslo, Adam R
Format: Artigo
Idioma:Inglês
Publicat: Beilstein-Institut 2013
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Full Research Paper
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3566858/
https://ncbi.nlm.nih.gov/pubmed/23400640
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3762/bjoc.9.3
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