Patterns of resistance development with integrase inhibitors in HIV

References

• BroderSThe development of antiretroviral therapy and its impact on the HIV-1/AIDS pandemicAntiviral Res201085111820018391
   PubMed Web of Science ®Google Scholar
• PalellaFJJrDelaneyKMMoormanACDeclining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV Outpatient Study InvestigatorsN Engl J Med1998338138538609516219
   PubMed Web of Science ®Google Scholar
• WalenskyRPPaltielADLosinaEThe survival benefits of AIDS treatment in the United StatesJ Infect Dis20061941111916741877
   PubMed Web of Science ®Google Scholar
• CihlarTRayASNucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudineAntiviral Res2010851395819887088
   PubMed Web of Science ®Google Scholar
• De BethuneMPNon-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of the last 20 years (1989–2009)Antiviral Res2010851759019781578
   PubMed Web of Science ®Google Scholar
• WensingAMvan MaarseveenNMNijhuisMFifteen years of HIV protease inhibitors: raising the barrier to resistanceAntiviral Res2010851597419853627
   PubMed Web of Science ®Google Scholar
• CraigieRHIV integrase, a brief overview from chemistry to therapeuticsJ Biol Chem200127626232132321611346660
   PubMed Web of Science ®Google Scholar
• EngelmanAReverse transcription and integrationKurthABannertNRetroviruses: Molecular Biology, Genomics and PathogenesisNorfolk (UK)Caister Academic Press2010129159
   Google Scholar
• HazudaDJFelockPWitmerMInhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cellsScience2000287545364665010649997
   PubMed Web of Science ®Google Scholar
• PommierYJohnsonAAMarchandCIntegrase inhibitors to treat HIV/AIDSNat Rev Drug Discov20054323624815729361
   PubMed Web of Science ®Google Scholar
• MarkowitzMNguyenBYGotuzzoEProtocol 004 Part II Study TeamRapid and durable antiretroviral effect of the HIV-1 integrase inhibitor raltegravir as part of combination therapy in treatment-naïve patients with HIV-1 infection: results of a 48-week controlled studyJ Acquir Immune Defic Syndr200746212513317721395
   PubMed Web of Science ®Google Scholar
• CooperDASteigbigelRTGatellJMBENCHMRK Study TeamsSubgroup and resistance analyses of raltegravir for resistant HIV-1 infectionN Engl J Med2008359435536518650513
   PubMed Web of Science ®Google Scholar
• SteigbigelRTCooperDAKumarPNBENCHMRK Study TeamsRaltegravir with optimized background therapy for resistant HIV-1 infectionN Engl J Med2008359433935418650512
   PubMed Web of Science ®Google Scholar
• BukrinskyMISharovaNMcDonaldTLPushkarskayaTTarpleyWGStevensonMAssociation of integrase, matrix, and reverse transcriptase antigens of human immunodeficiency virus type 1 with viral nucleic acids following acute infectionProc Natl Acad Sci U S A19939013612561297687060
   PubMed Web of Science ®Google Scholar
• MillerMDFarnetCMBushmanFDHuman immunodeficiency virus type 1 preintegration complexes: studies of organization and compositionJ Virol1997717538253909188609
   PubMed Web of Science ®Google Scholar
• BushmanFDHost proteins in retroviral cDNA integrationAdv Virus Res19995230131710384239
   PubMed Web of Science ®Google Scholar
• LinCWEngelmanAThe barrier-to-autointegration factor is a component of functional human immunodeficiency virus type 1 preintegration complexesJ Virol20037785030503612663813
   PubMed Web of Science ®Google Scholar
• RaghavendraNKShkriabaiNGrahamRLJHessSKvaratskheliaMWuLIdentification of host proteins associated with HIV-1 preintegration complexes isolated from infected CD4+ cellsRetrovirology201076620698996
   PubMed Web of Science ®Google Scholar
• WoodwardCLPrakobwanakitSMosessianSChowSAIntegrase interacts with nucleoporin NUP153 to mediate the nuclear import of human immunodeficiency virus type 1J Virol200983136522653319369352
   PubMed Web of Science ®Google Scholar
• YoderKEBushmanFDRepair of gaps in retroviral DNA integration intermediatesJ Virol20007423111911120011070016
   PubMed Web of Science ®Google Scholar
• SchroderARShinnPChenHBerryCEckerJRBushmanFHIV-1 integration in the human genome favors active genes and local hotspotsCell2002110452152912202041
   PubMed Web of Science ®Google Scholar
• MitchellRSBeitzelBFSchroderARRetroviral DNA integration: ASLV, HIV, and MLV show distinct target site preferencesPLoS Biol200428E23415314653
   PubMed Web of Science ®Google Scholar
• WuXBurgessSMIntegration target site selection for retroviruses and transposable elementsCell Mol Life Sci20046119–202588259615526164
   PubMed Web of Science ®Google Scholar
• MaxfieldLFFraizeCDCoffinJMRelationship between retroviral DNA-integration-site selection and host cell transcriptionProc Natl Acad Sci U S A200510251436144115659548
   PubMed Web of Science ®Google Scholar
• DydaFHickmanABJenkinsTMEngelmanACraigieRDaviesDRCrystal structure of the catalytic domain of HIV-1 integrase: similarity to other polynucleotidyl transferasesScience19942665193198119867801124
   PubMed Web of Science ®Google Scholar
• ChenJCKrucinskiJMierckeLJCrystal structure of the HIV-1 integrase catalytic core and C-terminal domains: a model for viral DNA bindingProc Natl Acad Sci U S A200097158233823810890912
   PubMed Web of Science ®Google Scholar
• WangJYLingHYangWCraigieRStructure of a two-domain fragment of HIV-1 integrase: implications for domain organization in the intact proteinEMBO J200120247333734311743009
   PubMed Web of Science ®Google Scholar
• McCollDJChenXStrand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapyAntiviral Res201085110111819925830
   PubMed Web of Science ®Google Scholar
• EngelmanAHickmanABCraigieRThe core and carboxyl-terminal domains of the integrase protein of human immunodeficiency virus type 1 each contribute to nonspecific DNA bindingJ Virol1994689591159178057470
   PubMed Web of Science ®Google Scholar
• KrishnanLLiXNaraharisettyHLHareSCherepanovPEngelmanAStructure-based modeling of the functional HIV-1 intasome and its inhibitionProc Natl Acad Sci U S A201010736159101591520733078
   PubMed Web of Science ®Google Scholar
• HareSGuptaSSValkovEEngelmanACherepanovPRetroviral intasome assembly and inhibition of DNA strand transferNature2010464728623223620118915
   PubMed Web of Science ®Google Scholar
• MarchandCMaddaliKMetifiotMPommierYHIV-1 IN inhibitors: 2010 update and perspectivesCurr Top Med Chem20099111016103719747122
   PubMed Web of Science ®Google Scholar
• KobayashiMNakaharaKSekiTSelection of diverse and clinically relevant integrase inhibitor-resistant human immunodeficiency virus type 1 mutantsAntiviral Res200880221322218625269
   PubMed Web of Science ®Google Scholar
• PacePRowleyMIntegrase inhibitors for the treatment of HIV infectionCurr Opin Drug Discov Devel2008114471479
   Google Scholar
• ShimuraKKodamaESakagamiYBroad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)J Virol200882276477417977962
   PubMed Web of Science ®Google Scholar
• GoodmanDHluhanichRWatersJIntegrase inhibitor resistance involves complex interactions among primary and secondary resistance mutations: a novel mutation L68V/I associates with E92Q and increases resistance [abstract]Antivir Ther200813Suppl 3A15
   Google Scholar
• FunAvan BaelenKvan LelyveldSFMutation Q95K enhances N155H-mediated integrase inhibitor resistance and improves viral replication capacityJ Antimicrob Chemother201065112300230420736234
   PubMed Web of Science ®Google Scholar
• FernsRBKirkSBennettJWilliamsIEdwardsSPillayDThe dynamics of appearance and disappearance of HIV-1 integrase mutations during and after withdrawal of raltegravir therapyAIDS200923162159216419571721
   PubMed Web of Science ®Google Scholar
• Ceccherini-SilbersteinFArmeniaDD’ArrigoRVirological response and resistance in multi-experienced patients treated with raltegravir [abstract]Antivir Ther200813Suppl 3A20
   Google Scholar
• CanducciFMarinozziMCSampaoloMGenotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravirJ Antimicrob Chemother201065342543320056687
   PubMed Web of Science ®Google Scholar
• MyersREPillayDAnalysis of natural sequence variation and covariation in human immunodeficiency virus type 1 integraseJ Virol200882189228923518596095
   PubMed Web of Science ®Google Scholar
• FransenSGuptaSDanovichRLoss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred via multiple non-overlapping genetic pathwaysJ Virol20098322114401144619759152
   PubMed Web of Science ®Google Scholar
• RheeSYLiuTFKiuchiMNatural variation of HIV-1 group M integrase: implications for a new class of antiretroviral inhibitorsRetrovirology200857418687142
   PubMed Web of Science ®Google Scholar
• DelelisOMaletINaLThe G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutationNucleic Acids Res20093741193120119129221
   PubMed Web of Science ®Google Scholar
• MaletIDelelisOSoulieCQuasispecies variant dynamics during emergence of resistance to raltegravir in HIV-1-infected patientsJ Antimicrob Chemother200963479580419221102
   PubMed Web of Science ®Google Scholar
• NakaharaKWakasa-MorimotoCKobayashiMSecondary mutations in viruses resistant to HIV-1 integrase inhibitors that restore viral infectivity and replication kineticsAntiviral Res200981214114619027039
   PubMed Web of Science ®Google Scholar
• MetifiotMMaddaliKNaumovaAZhangXMarchandCPommierYBiochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravirBiochemistry201049173715372220334344
   PubMed Web of Science ®Google Scholar
• ReigadasSAniesGMasquelierBThe HIV-1 integrase mutations Y143C/R are an alternative pathway for resistance to raltegravir and impact the enzyme functionsPLoS One201054e1031120436677
   PubMed Web of Science ®Google Scholar
• MaletIDelelisOValantinMAMutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitroAntimicrob Agents Chemother20085241351135818227187
   PubMed Web of Science ®Google Scholar
• GroblerJAStillmockKAMillerMDHazudaDJMechanism by which the HIV integrase active-site mutation N155H confers resistance to raltegravir [abstract]Antivir Ther200813Suppl 3A41
   Google Scholar
• DelelisOThierrySSubraFImpact of Y143 HIV-1 integrase mutations on resistance to raltegravir in vitro and in vivoAntimicrob Agents Chemother201054149150119901095
   PubMed Web of Science ®Google Scholar
• CharpentierCKarmochkineMLaureillardDDrug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapyHIV Med20089976577018651855
   PubMed Web of Science ®Google Scholar
• SichtigNSierraSKaiserREvolution of raltegravir resistance during therapyJ Antimicrob Chemother2009641253219447792
   PubMed Web of Science ®Google Scholar
• PradaNMarkowitzMNovel integrase inhibitors for HIVExpert Opin Investig Drugs201019910871098
   PubMed Web of Science ®Google Scholar
• UnderwoodMJohnsBSatoAFujiwaraTSpreenWS/GSK1349572: a next generation integrase inhibitor with activity against integrase inhibitor-resistant clinical isolates from patients experiencing virologic failure while on raltegravir therapy [abstract]5th IAS Conference on HIV Pathogenesis, Treatment and Prevention2009 Jul 19–22Cape Town, South Africa
   Google Scholar
• SatoAKobayashiMYoshinagaTS/GSK1349572 is a potent next generation HIV integrase inhibitor [abstract]5th IAS Conference on HIV Pathogenesis, Treatment and Prevention2009 Jul 19–22Cape Town, South Africa
   Google Scholar
• SekiTKobayashiMWakasa-MorimotoCS/GSK1349572 is a potent next generation HIV integrase inhibitor and demonstrates a superior resistance profile substantiated with 60 integrase mutant molecular clones [abstract]17th Conference on Retroviruses and Opportunistic Infections2010 Feb 16–19San Francisco, CA
   Google Scholar
• World Health Organization (WHO)Antiretroviral therapy for HIV infection in adults and adolescents: recommendations for a public health approach2010 Available from: http://whqlibdoc.who.int/publications/2010/9789241599764_eng.pdf. Accessed January 13, 2011.
   Google Scholar
• SteigbigelRTCooperDATepplerHBENCHMRK Study TeamsLong-term efficacy and safety of raltegravir combined with optimized background therapy in treatment-experienced patients with drug-resistant HIV infection: week 96 results of the BENCHMRK 1 and 2 Phase III trialsClin Infect Dis201050460561220085491
   PubMed Web of Science ®Google Scholar
• LennoxJLDeJesusELazzarinASTARTMRK InvestigatorsSafety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naïve patients with HIV-1 infection: a multicentre, double-blind randomised controlled trialLancet2009374969279680619647866
   PubMed Web of Science ®Google Scholar
• ReynesJLawalAPulidoFLopinavir/ritonavir combined with raltegravir demonstrated similar antiviral efficacy and safety as lopinavir/ritonavir combined with tenofovir disoproxil fumarate/emtricitabine in treatment-naïve HIV-1 infected subjects [abstract]XVIII International AIDS Conference2010 Jul 18–23Vienna, Austria
   Google Scholar
• KozalMLupoSDeJesusESPARTAN Study TeamThe SPARTAN study: a pilot study to assess the safety and efficacy of an investigational NRTI- and RTV-sparing regimen of atazanavir (ATV) experimental dose of 300 mg BID plus raltegravir (RAL) 400 mg BID (ATV+RAL) in treatment-naïve HIV-infected subjects [abstract]XVIII International AIDS Conference2010 Jul 18–23Vienna, Austria
   Google Scholar
• PowderlyWGIntegrase inhibitors in the treatment of HIV-1 infectionJ Antimicrob Chemother201065122485248820852268
   PubMed Web of Science ®Google Scholar
• CohenCShamblawDRuanePSinglet-tablet, fixed-dose regimen of elvitegravir/emtricitabine/tenofovir disoproxil fumarate/GS-9350 achieves a high rate of virologic suppression and GS-9350 is an effective booster [abstract]17th Conference on Retroviruses and Opportunistic Infections2010 Feb 16–19San Francisco, CA
   Google Scholar
• EronJJYoungBCooperDASWITCHMRK 1 and 2 InvestigatorsSwitch to a raltegravir-based regimen versus continuation of a lopinavir-ritonavir-based regimen in stable HIV-infected patients with suppressed viraemia (SWITCHMRK 1 and 2): two multicentre, double-blind, randomised controlled trialsLancet2010375971239640720074791
   PubMed Web of Science ®Google Scholar
• MartinezELarrousseMLlibreJMSPIRAL Study GroupSubstitution of raltegravir for ritonavir-boosted protease inhibitors in HIV-infected patients: the SPIRAL studyAIDS201024111697170720467288
   PubMed Web of Science ®Google Scholar
• FinziDBlanksonJSilicianoJDLatent infection of CD4+ T cells provides a mechanism for lifelong persistence of HIV-1, even in patients on effective combination therapyNat Med19995551251710229227
   PubMed Web of Science ®Google Scholar
• PalmerSMaldarelliFWiegandALow-level viremia persists for at least 7 years in patients on suppressive antiretroviral therapyProc Natl Acad Sci U S A2008105103879388418332425
   PubMed Web of Science ®Google Scholar
• CroteauDLetendreSBestBMCHARTER GroupTotal raltegravir concentrations in cerebrospinal fluid exceed the 50-percent inhibitory concentration for wild-type HIV-1Antimicrob Agents Chemother201054125156516020876368
   PubMed Web of Science ®Google Scholar
• ArchinNMCheemaMParkerDAntiretroviral intensification and valproic acid lack sustained effect on residual HIV-1 viremia or resting CD4+ cell infectionPLoS One201052e939020186346
   PubMed Web of Science ®Google Scholar
• GandhiRZhengSBoschRRaltegravir (RAL) intensification does not reduce low-level residual viremia in HIV-1-infected patients on antiretroviral therapy (ART): results from ACTG A5244 [abstract]5th IAS Conference on HIV Pathogenesis, Treatment and Prevention2009 Jul 19–22Cape Town, South Africa
   Google Scholar
• GoethalsOVosAvan GinderenMPrimary 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 profilesVirology2010402233834620421122
   PubMed Web of Science ®Google Scholar
• AniesGDa SilvaDRecordon-PinsonPClonal analysis of raltegravir-resistant patterns including mutations at positions 143 and 155 [abstract]16th Conference on Retroviruses and Opportunistic Infections2009 Feb 8–11Montreal, Canada
   Google Scholar
• GoethalsOClaytonRvan GinderenMResistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitorsJ Virol20088221103661037418715920
   PubMed Web of Science ®Google Scholar
• MillerMDDanovichRMKeYon behalf of the P005 Study TeamLongitudinal analysis of resistance to the HIV-1 integrase inhibitor raltegravir: results from P005, a phase II study in treatment-experienced patients [abstract]Antivir Ther200813Suppl 3A8
   Google Scholar
• HuZKuritzkesDREffect of raltegravir resistance mutations in HIV-1 integrase on viral fitnessJ Acquir Immune Defic Syndr201055214815520634701
   PubMed Web of Science ®Google Scholar
• GerettiAMFearnhillECeccherini-SilbersteinFPrevalence and patterns of raltegravir resistance in treated patients in Europe [abstract]Antivir Ther201015Suppl 2A62
   Google Scholar
• BlancoJLBuzonMJCalvoMEvolution of viral load and integrase resistance mutations after interrupting raltegravir (RAL) in HIV-infected subjects with virological failure on a RAL-containing regimen: the Raldyn study [abstract]Antivir Ther201015Suppl 2A133
   Google Scholar
• BaldantiFPaolucciSGulminettiRBrandoliniMBarbariniGMaseratiREarly emergence of raltegravir resistance mutations in patients receiving HAART salvage regimensJ Med Virol201082111612219950236
   PubMed Web of Science ®Google Scholar
• McCollDJFransenSGuptaSResistance and cross-resistance to first generation integrase inihibitors: insights from a Phase II study of elvitegravir (GS-9137) [abstract]Antivir Ther200712Suppl 1S11
   Google Scholar
• GallienSDelaugerreCHuZIntegrase inhibitor resistance mutations in treatment-experienced HIV-1-infected patients with low-level viraemia receiving raltegravir-containing antiretroviral therapy: an ANRS 138-EASIER Trial substudy [abstract]Antivir Ther201015Suppl 2A60
   Google Scholar