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Article

Structural Adaptation of Darunavir Analogues against Primary Mutations in HIV-1 Protease.

ACS infectious diseases - 8 Feb 2019

Lockbaum Gordon J, Leidner Florian, Rusere Linah N, Henes Mina, Kosovrasti Klajdi, Nachum Gily S, Nalivaika Ellen A, Ali Akbar, Yilmaz Nese Kurt, Schiffer Celia A

Abstract excerpt

HIV-1 protease is one of the prime targets of agents used in antiretroviral therapy against HIV. However, under selective pressure of protease inhibitors, primary mutations at the active site weaken inhibitor binding to confer resistance. Darunavir (DRV) is the most potent HIV-1 protease inhibitor in clinic; resistance is limited, as DRV fits well within the substrate envelope. Nevertheless, resistance is...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 30543749
DOI: 10.1021/acsinfecdis.8b00336
PMCID: PMC6941150

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