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Competitive fitness assays indicate that the E138A substitution in HIV-1 reverse transcriptase decreases in vitro susceptibility to emtricitabine.

作者信息

Sluis-Cremer Nicolas, Huber Kelly D, Brumme Chanson J, Harrigan P Richard

机构信息

University of Pittsburgh, Department of Medicine, Division of Infectious Diseases, Pittsburgh, Pennsylvania, USA.

出版信息

Antimicrob Agents Chemother. 2014;58(4):2430-3. doi: 10.1128/AAC.02114-13. Epub 2014 Jan 13.

Abstract

We characterized the relative fitness of multiple nonnucleoside reverse transcriptase (RT) inhibitor (NNRTI)-resistant HIV-1 variants in the presence of etravirine (ETV), rilpivirine (RPV), and/or the nucleoside RT inhibitor emtricitabine (FTC) by simultaneous competitive culture and 454 deep sequencing. The E138A substitution, typically associated with decreased virologic responses to ETV- and RPV-containing regimens, confers a clear fitness advantage to the virus in the presence of FTC and decreases FTC susceptibility 4.7-fold.

摘要

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TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
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