ArticleAIDS (London, England)2011
Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143.
Article in AIDS (London, England), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed.
- Review
- Mortality using raltegravir versus other integrase strand-transfer inhibitors in people with HIV in Europe and Australia: a prospective multicentre study.EClinicalMedicine · 2025Article
- Novel Dolutegravir and Lenacapavir Resistance Patterns in Human Immunodeficiency Virus Type 2 Infection: A Case Report.Open forum infectious diseases · 2025Article
- Discovery of Novel Integrase Inhibitors Acting outside the Active Site Through High-Throughput Screening.Molecules (Basel, Switzerland) · 2019Article
- Multifaceted HIV integrase functionalities and therapeutic strategies for their inhibition.The Journal of biological chemistry · 2019Review
- Structure-function analyses unravel distinct effects of allosteric inhibitors of HIV-1 integrase on viral maturation and integration.The Journal of biological chemistry · 2018Article
- Impact of the HIV-1 genetic background and HIV-1 population size on the evolution of raltegravir resistance.Retrovirology · 2018Article
- HIV-1 Resistance to Dolutegravir Is Affected by Cellular Histone Acetyltransferase Activity.Journal of virology · 2017Article
- HIV drug resistance against strand transfer integrase inhibitors.Retrovirology · 2017Review
- Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase.European journal of medicinal chemistry · 2016Article
- A Novel Assay for Screening Inhibitors Targeting HIV Integrase LEDGF/p75 Interaction Based on Ni(2+) Coated Magnetic Agarose Beads.Scientific reports · 2016Article
- Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site.Nucleic acids research · 2016Article
- A novel assay for screening inhibitors targeting HIV-1 integrase dimerization based on Ni-NTA magnetic agarose beads.Scientific reports · 2016Article
- HIV-1 Integrase Strand Transfer Inhibitors with Reduced Susceptibility to Drug Resistant Mutant Integrases.ACS chemical biology · 2016Article
- A targeted DNA substrate mechanism for the inhibition of HIV-1 integrase by inhibitors with antiretroviral activity.FEBS open bio · 2016Article
- Methods for the Analyses of Inhibitor-Induced Aberrant Multimerization of HIV-1 Integrase.Methods in molecular biology (Clifton, N.J.) · 2016Article
- HIV-1 integrase multimerization as a therapeutic target.Current topics in microbiology and immunology · 2015Review
- The mechanism of H171T resistance reveals the importance of Nδ-protonated His171 for the binding of allosteric inhibitor BI-D to HIV-1 integrase.Retrovirology · 2014Article
- Effect of HIV-1 integrase resistance mutations when introduced into SIVmac239 on susceptibility to integrase strand transfer inhibitors.Journal of virology · 2014Article
- Pharmacokinetics and dose-range finding toxicity of a novel anti-HIV active integrase inhibitor.Antiviral research · 2014Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
objectiveIn this study, we characterized elvitegravir activity in the context of raltegravir resistance mutations.
designUsing 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.
methodsRecombinant proteins were used in gel-based assays. Antiviral data were obtained with reporter viruses in a single-round infection using a luciferase-based assay.
resultsAlthough 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.
conclusionIn 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.
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