G118R and F121Y mutations identified in patients failing raltegravir treatment confer dolutegravir resistance

Comparative replication capacity of raltegravir-resistant strains and antiviral activity of the new-generation integrase inhibitor dolutegravir in human primary macrophages and lymphocytes

(2014) M. Pollicita et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

New raltegravir resistance pathways induce broad cross-resistance to all currently used integrase inhibitors

(2014) I. Malet et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Dolutegravir in Antiretroviral-Experienced Patients With Raltegravir- and/or Elvitegravir-Resistant HIV-1: 24-Week Results of the Phase III VIKING-3 Study

(2014) A. Castagna et al.   JOURNAL OF INFECTIOUS DISEASES

Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naive adults with HIV-1 infection (FLAMINGO): 48 week results from the randomised open-label phase 3b study

(2014) Bonaventura Clotet et al.   LANCET

In vitro phenotypes to elvitegravir and dolutegravir in primary macrophages and lymphocytes of clonal recombinant viral variants selected in patients failing raltegravir

(2013) F. Canducci et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study

(2013) Francois Raffi et al.   LANCET

Dolutegravir plus Abacavir–Lamivudine for the Treatment of HIV-1 Infection

(2013) Sharon L. Walmsley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Quantitative analysis of the time-course of viral DNA forms during the HIV-1 life cycle

(2013) Soundasse Munir et al.   Retrovirology

Broad Phenotypic Cross-Resistance to Elvitegravir in HIV-Infected Patients Failing on Raltegravir-Containing Regimens

(2012) Carolina Garrido et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Elvitegravir: a once-daily inhibitor of HIV-1 integrase

(2012) Todd Wills et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks

(2012) Paul E Sax et al.   LANCET

Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial

(2012) Edwin DeJesus et al.   LANCET

The structural biology of HIV-1: mechanistic and therapeutic insights

(2012) Alan Engelman et al.   NATURE REVIEWS MICROBIOLOGY

Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium

(2011) Bach-Yen T. Nguyen et al.   Annals of the New York Academy of Sciences

Dolutegravir (S/GSK1349572) Exhibits Significantly Slower Dissociation than Raltegravir and Elvitegravir from Wild-Type and Integrase Inhibitor-Resistant HIV-1 Integrase-DNA Complexes

(2011) Kendra E. Hightower et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Resistance to raltegravir highlights integrase mutations at codon 148 in conferring cross-resistance to a second-generation HIV-1 integrase inhibitor

(2011) Olivia Goethals et al.   ANTIVIRAL RESEARCH

Characterization of the R263K Mutation in HIV-1 Integrase That Confers Low-Level Resistance to the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir

(2011) P. K. Quashie et al.   JOURNAL OF VIROLOGY

Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study

(2011) Jean-Michel Molina et al.   LANCET INFECTIOUS DISEASES

Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572)

(2011) S. Hare et al.   MOLECULAR PHARMACOLOGY

In VitroAntiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor

(2010) Masanori Kobayashi et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Identification of Novel Mutations Responsible for Resistance to MK-2048, a Second-Generation HIV-1 Integrase Inhibitor

(2010) T. Bar-Magen et al.   JOURNAL OF VIROLOGY

The mechanism of retroviral integration from X-ray structures of its key intermediates

(2010) Goedele N. Maertens et al.   NATURE

Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance

(2010) S. Hare et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to first-generation integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles

(2010) Olivia Goethals et al.   VIROLOGY

Impact of Y143 HIV-1 Integrase Mutations on Resistance to Raltegravir In Vitro and In Vivo

(2009) O. Delelis et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation

(2009) O. Delelis et al.   NUCLEIC ACIDS RESEARCH

Raltegravir, elvitegravir, and metoogravir: the birth of "me-too" HIV-1 integrase inhibitors

(2009) Erik Serrao et al.   Retrovirology

Mutations Associated with Failure of Raltegravir Treatment Affect Integrase Sensitivity to the Inhibitor In Vitro

(2008) I. Malet et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Secondary mutations in viruses resistant to HIV-1 integrase inhibitors that restore viral infectivity and replication kinetics

(2008) Koichiro Nakahara et al.   ANTIVIRAL RESEARCH

Comparison of Raltegravir and Elvitegravir on HIV-1 Integrase Catalytic Reactions and on a Series of Drug-Resistant Integrase Mutants†

(2008) Jessica Marinello et al.   BIOCHEMISTRY

Resistance Mutations in Human Immunodeficiency Virus Type 1 Integrase Selected with Elvitegravir Confer Reduced Susceptibility to a Wide Range of Integrase Inhibitors

(2008) O. Goethals et al.   JOURNAL OF VIROLOGY

Subgroup and Resistance Analyses of Raltegravir for Resistant HIV-1 Infection

(2008) David A. Cooper et al.   NEW ENGLAND JOURNAL OF MEDICINE

Integrase and integration: biochemical activities of HIV-1 integrase

(2008) Olivier Delelis et al.   Retrovirology