Article
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
Journal of medicinal chemistry - 12 Apr 2012
Chang Yu-Chung E, Yu XiaXia, Zhang Ying, Tie Yunfeng, Wang Yuan-Fang, Yashchuk Sofiya, Ghosh Arun K, Harrison Robert W, Weber Irene T
Abstract excerpt
GRL-02031 (1) is an HIV-1 protease (PR) inhibitor containing a novel P1' (R)-aminomethyl-2-pyrrolidinone group. Crystal structures at resolutions of 1.25-1.55 Å were analyzed for complexes of 1 with the PR containing major drug resistant mutations, PR(I47V), PR(L76V), PR(V82A), and PR(N88D). Muta...
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