Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases

We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of T. brucei brucei parasites in culture. A high resolution (1.75Å) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such...

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Detalhes bibliográficos
Main Authors: Bryant, Clifford, Kerr, Iain D., Debnath, Moumita, Kenny, K. H. Ang, Ratnam, Joseline, Ferreira, Rafaela S., Jaishankar, Priyadarshini, Zhao, DongMei, Arkin, Michelle R., McKerrow, James H., Brinen, Linda S., Renslo, Adam R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2009
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3760505/
https://ncbi.nlm.nih.gov/pubmed/19773167
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2009.08.098
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