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Novel HIV PR inhibitors with C4-substituted bis-THF and bis-fluoro-benzyl target the two active site mutations of highly drug resistant mutant PR(S17)

The emergence of multidrug resistant (MDR) HIV strains severely reduces the effectiveness of antiretroviral therapy. Clinical inhibitor darunavir (1) has picomolar binding affinity for HIV-1 protease (PR), however, drug resistant variants like PR(S17) show poor inhibition by 1, despite the presence...

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Vydáno v:Biochem Biophys Res Commun
Hlavní autoři: Agniswamy, Johnson, Kneller, Daniel W., Ghosh, Arun K., Weber, Irene T.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2021
Témata:
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC8286348/
https://ncbi.nlm.nih.gov/pubmed/34111669
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bbrc.2021.05.094
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