Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1′-pyrrolidinone ring

GRL-02031 (1) is an HIV-1 protease (PR) inhibitor containing a novel P1′ (R)-aminomethyl-2-pyrrolidinone group. Crystal structures at resolutions of 1.25 to 1.55 Å were analyzed for complexes of 1 with the PR containing major drug resistant mutations, PR(I47V), PR(L76V), PR(V82A) and PR(N88D). Mutat...

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Main Authors: Chang, Yu Chung E., Yu, XiaXia, Zhang, Ying, Tie, Yunfeng, Wang, Yuan Fang, Yashchuk, Sofiya, Ghosh, Arun K., Harrison, Robert W., Weber, Irene T.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3355519/
https://ncbi.nlm.nih.gov/pubmed/22401672
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300072d
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