期刊
AIDS
卷 25, 期 9, 页码 1175-1178出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/QAD.0b013e3283473599
关键词
elvitegravir; HIV-1; integrase inhibitor; integrase resistance; raltegravir
资金
- NIH, National Cancer Institute (NCI), Center for Cancer Research (CCR) [Z01BC007333-09LMP]
- IATAP (Intramural AIDS Target Antiviral Program)
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. Conclusion: In addition to favorable pharmacokinetics compared to raltegravir, our findings provide the rationale for using elvitegravir in patients failing raltegravir because of the integrase mutation Y143. (C) 2011 Wolters Kluwer Health | Lippincott Williams & Wilkins
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