Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143.

ABSTRACT:

Objective

In this study, we characterized elvitegravir activity in the context of raltegravir resistance mutations.

Design

Using site-directed mutagenesis, we generated recombinant integrase proteins and viruses harboring raltegravir resistance mutation to assess the biochemical and cellular activity of elvitegravir in the presence of such mutants.

Methods

Recombinant proteins were used in gel-based assays. Antiviral data were obtained with reporter viruses in a single-round infection using a luciferase-based assay.

Results

Although main raltegravir resistance pathways involving mutations at integrase position 148 and 155 confer cross-resistance to elvitegravir, elvitegravir remains fully active against the Y143R mutant integrase and virus particles.

Conclus

SUBMITTER: Metifiot M 

PROVIDER: S-EPMC7380719 | biostudies-literature | 2011 Jun

REPOSITORIES: biostudies-literature