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[4]CurrentPatentAssignee:VIATRISINC-WO2011/4389,2011,A2Locationinpatent:Page/Pagecolumn36
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[2]CurrentPatentAssignee:ADVENTINTERNATIONALCORPORATION-WO2014/56465,2014,A1Locationinpatent:Page/Pagecolumn21;22
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[5]Rádl,Stanislav;Stach,Jan;Píša,Ondřej;Cinibulk,Josef;Havlíček,Jaroslav;Zajícová,Markéta;Pekárek,Tomáš[JournalofHeterocyclicChemistry,2016,vol.53,#6,p.1738-1749]
[1]Sato,Motohide;Motomura,Takahisa;Aramaki,Hisateru;Matsuda,Takashi;Yamashita,Masaki;Ito,Yoshiharu;Kawakami,Hiroshi;Matsuzaki,Yuji;Watanabe,Wataru;Yamataka,Kazunobu;Ikeda,Satoru;Kodama,Eiichi;Matsuoka,Masao;Shinkai,Hisashi[JournalofMedicinalChemistry,2006,vol.49,#5,p.1506-1508]
[2]Rádl,Stanislav;Stach,Jan;Píša,Ondřej;Cinibulk,Josef;Havlíček,Jaroslav;Zajícová,Markéta;Pekárek,Tomáš[JournalofHeterocyclicChemistry,2016,vol.53,#6,p.1738-1749]
[3]Rádl,Stanislav;Stach,Jan;Píša,Ondřej;Cinibulk,Josef;Havlíček,Jaroslav;Zajícová,Markéta;Pekárek,Tomáš[JournalofHeterocyclicChemistry,2016,vol.53,#6,p.1738-1749]
[4]Rádl,Stanislav;Stach,Jan;Píša,Ondřej;Cinibulk,Josef;Havlíček,Jaroslav;Zajícová,Markéta;Pekárek,Tomáš[JournalofHeterocyclicChemistry,2016,vol.53,#6,p.1738-1749]
[5]Rádl,Stanislav;Stach,Jan;Píša,Ondřej;Cinibulk,Josef;Havlíček,Jaroslav;Zajícová,Markéta;Pekárek,Tomáš[JournalofHeterocyclicChemistry,2016,vol.53,#6,p.1738-1749]
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[5]CurrentPatentAssignee:VIATRISINC-WO2011/4389,2011,A2
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[9]CurrentPatentAssignee:JAPANTOBACCOINC-WO2005/113508,2005,A1
[10]CurrentPatentAssignee:JAPANTOBACCOINC-WO2005/113508,2005,A1
Title: Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA.
Journal: Bioorganic & medicinal chemistry 20160901
Title: Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection.
Journal: Antimicrobial agents and chemotherapy 20150101
Title: Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
Journal: Journal of medicinal chemistry 20140424
Title: Impact of primary elvitegravir resistance-associated mutations in HIV-1 integrase on drug susceptibility and viral replication fitness.
Journal: Antimicrobial agents and chemotherapy 20130601
Title: A novel anti-HIV active integrase inhibitor with a favorable in vitro cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferase metabolism profile.
Journal: Antiviral research 20130601
Title: Carbamoyl pyridone HIV-1 integrase inhibitors. 2. Bi- and tricyclic derivatives result in superior antiviral and pharmacokinetic profiles.
Journal: Journal of medicinal chemistry 20130214
Title: Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors.
Journal: Journal of inorganic biochemistry 20130101
Title: The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes.
Journal: PLoS pathogens 20130101
Title: Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage.
Journal: Retrovirology 20130101
Title: Carbamoyl pyridone HIV-1 integrase inhibitors. 1. Molecular design and establishment of an advanced two-metal binding pharmacophore.
Journal: Journal of medicinal chemistry 20121025
Title: Antiviral drug advances in the treatment of human immunodeficiency virus (HIV) and chronic hepatitis C virus (HCV).
Journal: Current opinion in pharmacology 20121001
Title: The future of integrase inhibitors of HIV-1.
Journal: Current opinion in virology 20121001
Title: The development of novel HIV integrase inhibitors and the problem of drug resistance.
Journal: Current opinion in virology 20121001
Title: Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors.
Journal: Molecules (Basel, Switzerland) 20120906
Title: Drug resistance mutations of HIV type 1 non-B viruses to integrase inhibitors in treatment-naive patients from sub-saharan countries and discordant interpretations.
Journal: AIDS research and human retroviruses 20120901
Title: Effect of cobicistat on glomerular filtration rate in subjects with normal and impaired renal function.
Journal: Journal of acquired immune deficiency syndromes (1999) 20120901
Title: The use of HIV-1 integrase inhibitors in antiretroviral naive patients.
Journal: Current opinion in HIV and AIDS 20120901
Title: Pharmacology of HIV integrase inhibitors.
Journal: Current opinion in HIV and AIDS 20120901
Title: Combinational therapies for HIV: a focus on EVG/COBI/FTC/TDF.
Journal: Expert opinion on pharmacotherapy 20120901
Title: HIV integrase inhibitors in ART-experienced patients.
Journal: Current opinion in HIV and AIDS 20120901
Title: Tolerability of HIV integrase inhibitors.
Journal: Current opinion in HIV and AIDS 20120901
Title: [A single tablet against HIV: new combination preparation improves therapy].
Journal: Deutsche medizinische Wochenschrift (1946) 20120801
Title: In-vivo selection of the mutation F121Y in a patient failing raltegravir containing salvage regimen.
Journal: Antiviral research 20120701
Title: The elvitegravir Quad pill: the first once-daily dual-target anti-HIV tablet.
Journal: Expert opinion on investigational drugs 20120701
Title: Tenofovir: quo vadis anno 2012 (where is it going in the year 2012)?
Journal: Medicinal research reviews 20120701
Title: Update on raltegravir and the development of new integrase strand transfer inhibitors.
Journal: Southern medical journal 20120701
Title: 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.
Journal: Lancet (London, England) 20120630
Title: 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.
Journal: Lancet (London, England) 20120630
Title: Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors.
Journal: Journal of biomolecular screening 20120601
Title: A review of the virological efficacy of the 4 World Health Organization-recommended tenofovir-containing regimens for initial HIV therapy.
Journal: Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 20120315
Title: Elvitegravir: a once-daily inhibitor of HIV-1 integrase.
Journal: Expert opinion on investigational drugs 20120301
Title: Homology model-guided 3D-QSAR studies of HIV-1 integrase inhibitors.
Journal: Journal of chemical information and modeling 20120227
Title: In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4.
Journal: Antiviral research 20120201
Title: 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.
Journal: The Lancet. Infectious diseases 20120101
Title: Elvitegravir: a once daily alternative to raltegravir.
Journal: The Lancet. Infectious diseases 20120101
Title: Elvitegravir: a once-daily, boosted, HIV-1 integrase inhibitor.
Journal: Expert review of anti-infective therapy 20120101
Title: Diketoacid inhibitors of HIV-1 integrase: from L-708,906 to raltegravir and beyond.
Journal: Current medicinal chemistry 20120101
Title: Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings.
Journal: HIV/AIDS (Auckland, N.Z.) 20120101
Title: The use of preexposure treatments for HIV prophylaxis.
Journal: HIV/AIDS (Auckland, N.Z.) 20120101
Title: Genetic barrier to the development of resistance to integrase inhibitors in HIV-1 subtypes CRF01_AE and B.
Journal: Intervirology 20120101
Title: Incomplete immune recovery in HIV infection: mechanisms, relevance for clinical care, and possible solutions.
Journal: Clinical & developmental immunology 20120101
Title: BF integrase genes of HIV-1 circulating in São Paulo, Brazil, with a recurrent recombination region.
Journal: PloS one 20120101
Title: Novel therapeutic strategies targeting HIV integrase.
Journal: BMC medicine 20120101
Title: Antiretroviral drugs: critical issues and recent advances.
Journal: Indian journal of pharmacology 20120101
Title: Development of elvitegravir resistance and linkage of integrase inhibitor mutations with protease and reverse transcriptase resistance mutations.
Journal: PloS one 20120101
Title: In Silico and In Vitro Comparison of HIV-1 Subtypes B and CRF02_AG Integrases Susceptibility to Integrase Strand Transfer Inhibitors.
Journal: Advances in virology 20120101
Title: Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens.
Journal: PloS one 20120101
Title: Investigating the role of metal chelation in HIV-1 integrase strand transfer inhibitors.
Journal: Journal of medicinal chemistry 20111222
Title: The HIV-1 integrase G118R mutation confers raltegravir resistance to the CRF02_AG HIV-1 subtype.
Journal: The Journal of antimicrobial chemotherapy 20111201
Title: Recent advances in antiretroviral treatment and prevention in HIV-infected patients.
Journal: Current opinion in HIV and AIDS 20111201
Title: HIV-1 integrase inhibitors: a review of their chemical development.
Journal: Antiviral chemistry & chemotherapy 20111117
Title: 3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1.
Journal: Expert opinion on therapeutic patents 20111101
Title: Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors.
Journal: Bioorganic & medicinal chemistry 20110915
Title: Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity.
Journal: Bioorganic & medicinal chemistry 20110815
Title: Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors.
Journal: Molecules (Basel, Switzerland) 20110811
Title: New first and second generation inhibitors of human immunodeficiency virus-1 integrase.
Journal: Expert opinion on therapeutic patents 20110801
Title: Resistance to raltegravir highlights integrase mutations at codon 148 in conferring cross-resistance to a second-generation HIV-1 integrase inhibitor.
Journal: Antiviral research 20110801
Title: Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143.
Journal: AIDS (London, England) 20110601
Title: Binding modes of diketo-acid inhibitors of HIV-1 integrase: a comparative molecular dynamics simulation study.
Journal: Journal of molecular graphics & modelling 20110601
Title: HIV-1 integrase inhibitor resistance and its clinical implications.
Journal: The Journal of infectious diseases 20110501
Title: Foamy virus biology and its application for vector development.
Journal: Viruses 20110501
Title: Clinical pharmacokinetic and pharmacodynamic profile of the HIV integrase inhibitor elvitegravir.
Journal: Clinical pharmacokinetics 20110401
Title: Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro.
Journal: The Journal of antimicrobial chemotherapy 20110401
Title: Clinical management of HIV drug resistance.
Journal: Viruses 20110401
Title: Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection.
Journal: AIDS (London, England) 20110327
Title: Allosteric inhibitor development targeting HIV-1 integrase.
Journal: ChemMedChem 20110207
Title: In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
Journal: Antimicrobial agents and chemotherapy 20110201
Title: HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation.
Journal: European journal of medicinal chemistry 20110201
Title: 6-Benzylamino 4-oxo-1,4-dihydro-1,8-naphthyridines and 4-oxo-1,4-dihydroquinolines as HIV integrase inhibitors.
Journal: Bioorganic & medicinal chemistry letters 20110115
Title: Recent advances in antiretroviral drugs.
Journal: Expert opinion on pharmacotherapy 20110101
Title: K70Q adds high-level tenofovir resistance to 'Q151M complex' HIV reverse transcriptase through the enhanced discrimination mechanism.
Journal: PloS one 20110101
Title: Driving a decade of change: HIV/AIDS, patents and access to medicines for all.
Journal: Journal of the International AIDS Society 20110101
Title: HIV integrase variability and genetic barrier in antiretroviral naïve and experienced patients.
Journal: Virology journal 20110101
Title: Antiretroviral Therapy for HIV-2 Infection: Recommendations for Management in Low-Resource Settings.
Journal: AIDS research and treatment 20110101
Title: Patterns of resistance development with integrase inhibitors in HIV.
Journal: Infection and drug resistance 20110101
Title: HIV-2 integrase variation in integrase inhibitor-naïve adults in Senegal, West Africa.
Journal: PloS one 20110101
Title: G140S/Q148R and N155H mutations render HIV-2 Integrase resistant to raltegravir whereas Y143C does not.
Journal: Retrovirology 20110101
Title: A crystal structure of the catalytic core domain of an avian sarcoma and leukemia virus integrase suggests an alternate dimeric assembly.
Journal: PloS one 20110101
Title: Pathogenicity and rapid growth kinetics of feline immunodeficiency virus are linked to 3' elements.
Journal: PloS one 20110101
Title: In-silico Comparative Study and Quantitative Structure-activity Relationship Analysis of Some Structural and Physiochemical Descriptors of Elvitegravir Analogs.
Journal: Journal of young pharmacists : JYP 20110101
Title: Role of raltegravir in the management of HIV-1 infection.
Journal: HIV/AIDS (Auckland, N.Z.) 20110101
Title: Clinical Use of Inhibitors of HIV-1 Integration: Problems and Prospects.
Journal: Acta naturae 20110101
Title: Comparison of the Mechanisms of Drug Resistance among HIV, Hepatitis B, and Hepatitis C.
Journal: Viruses 20101201
Title: Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors.
Journal: Viruses 20101201
Title: Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV.
Journal: Journal of acquired immune deficiency syndromes (1999) 20101101
Title: Mutation Q95K enhances N155H-mediated integrase inhibitor resistance and improves viral replication capacity.
Journal: The Journal of antimicrobial chemotherapy 20101101
Title: Specific HIV-1 integrase polymorphisms change their prevalence in untreated versus antiretroviral-treated HIV-1-infected patients, all naive to integrase inhibitors.
Journal: The Journal of antimicrobial chemotherapy 20101101
Title: Development of integrase inhibitors of quinolone acid derivatives for treatment of AIDS: an overview.
Journal: Mini reviews in medicinal chemistry 20101001
Title: Physical trapping of HIV-1 synaptic complex by different structural classes of integrase strand transfer inhibitors.
Journal: Biochemistry 20100928
Title: HIV-1 subtype B and C integrase enzymes exhibit differential patterns of resistance to integrase inhibitors in biochemical assays.
Journal: AIDS (London, England) 20100910
Title: Novel antiretroviral combinations in treatment-experienced patients with HIV infection: rationale and results.
Journal: Drugs 20100910
Title: Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor.
Journal: Journal of virology 20100901
Title: Novel integrase inhibitors for HIV.
Journal: Expert opinion on investigational drugs 20100901
Title: Bunyaviridae RNA polymerases (L-protein) have an N-terminal, influenza-like endonuclease domain, essential for viral cap-dependent transcription.
Journal: PLoS pathogens 20100901
Title: Evolution of integrase resistance during failure of integrase inhibitor-based antiretroviral therapy.
Journal: Journal of acquired immune deficiency syndromes (1999) 20100801
Title: 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.
Journal: Virology 20100705
Title: Tautomerism and magnesium chelation of HIV-1 integrase inhibitors: a theoretical study.
Journal: ChemMedChem 20100705
Title: Resistance to integrase inhibitors.
Journal: Viruses 20100701
Title: HIV-1 resistance patterns to integrase inhibitors in antiretroviral-experienced patients with virological failure on raltegravir-containing regimens.
Journal: The Journal of antimicrobial chemotherapy 20100601
Title: Biochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravir.
Journal: Biochemistry 20100504
Title: Retrovirus Integrase-DNA Structure Elucidates Concerted Integration Mechanisms.
Journal: Viruses 20100501
Title: Natural polymorphisms of integrase among HIV type 1-infected South African patients.
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Title: Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV Type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial.
Journal: The Journal of infectious diseases 20100315
Title: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity.
Journal: Clinical pharmacology and therapeutics 20100301
Title: Single-tablet Quad regimen achieves high rate of virologic suppression.
Journal: AIDS patient care and STDs 20100301
Title: Pharmacokinetic interaction of ritonavir-boosted elvitegravir and maraviroc.
Journal: Journal of acquired immune deficiency syndromes (1999) 20100201
Title: Pharmacokinetics and drug-drug interactions of antiretrovirals: an update.
Journal: Antiviral research 20100101
Title: Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy.
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Title: Integrase inhibitors: a novel class of antiretroviral agents.
Journal: The Annals of pharmacotherapy 20100101
Title: Improving first-line antiretroviral therapy in resource-limited settings.
Journal: Current opinion in HIV and AIDS 20100101
Title: Genetic diversity on the integrase region of the pol gene among HIV type 1-infected patients naive for integrase inhibitors in São Paulo City, Brazil.
Journal: AIDS research and human retroviruses 20100101
Title: Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy.
Journal: Retrovirology 20100101
Title: [Analysis of HIV-1 integrase gene polymorphism in an HIV-infected population from the nosocomial outbreak of HIV infection in the south of Russia in 1989].
Journal: Voprosy virusologii 20100101
Title: The HIV-1 integrase mutations Y143C/R are an alternative pathway for resistance to Raltegravir and impact the enzyme functions.
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Title: 5th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention: summary of key research and implications for policy and practice - clinical sciences.
Journal: Journal of the International AIDS Society 20100101
Title: Anticipating and blocking HIV-1 escape by second generation antiviral shRNAs.
Journal: Retrovirology 20100101
Title: Resistance to HIV-1 integrase inhibitors: A structural perspective.
Journal: Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 20100101
Title: Susceptibility of the human retrovirus XMRV to antiretroviral inhibitors.
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Title: Polymorphisms of HIV-2 integrase and selection of resistance to raltegravir.
Journal: Retrovirology 20100101
Title: The HIV-1 integrase α4-helix involved in LTR-DNA recognition is also a highly antigenic peptide element.
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Title: Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy.
Journal: Infection and drug resistance 20100101
Title: Role of etravirine in the management of treatment-experienced patients with human immunodeficiency virus type 1.
Journal: HIV/AIDS (Auckland, N.Z.) 20100101
Title: A combined genotypic and phenotypic human immunodeficiency virus type 1 recombinant virus assay for the reverse transcriptase and integrase genes.
Journal: Journal of virological methods 20091101
Title: Efavirenz: a decade of clinical experience in the treatment of HIV.
Journal: The Journal of antimicrobial chemotherapy 20091101
Title: Integrase inhibitors in salvage therapy regimens for HIV-1 infection.
Journal: Current opinion in HIV and AIDS 20091101
Title: Resistance to novel drug classes.
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Title: Elvitegravir: a new HIV integrase inhibitor.
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Title: In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer.
Journal: Future medicinal chemistry 20091001
Title: Induced-fit docking approach provides insight into the binding mode and mechanism of action of HIV-1 integrase inhibitors.
Journal: ChemMedChem 20090901
Title: Quinolone carboxylic acids as a novel monoketo acid class of human immunodeficiency virus type 1 integrase inhibitors.
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Title: Human immunodeficiency virus: 25 years of diagnostic and therapeutic strategies and their impact on hepatitis B and C virus.
Journal: Medical microbiology and immunology 20090801
Title: Analysis of binding parameters of HIV-1 integrase inhibitors: correlates of drug inhibition and resistance.
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Title: Lack of primary mutations associated with integrase inhibitors among HIV-1 subtypes B, C, and F circulating in Brazil.
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Title: Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
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Title: Analysis of pol integrase sequences in diverse HIV type 1 strains using a prototype genotyping assay.
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Title: Data demonstrate pharmacokinetic boosting activity of GS 9350.
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Title: Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant.
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Title: Elvitegravir, an oral HIV integrase inhibitor, for the potential treatment of HIV infection.
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Title: Dose-response of ritonavir on hepatic CYP3A activity and elvitegravir oral exposure.
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Title: Emerging pharmacology: inhibitors of human immunodeficiency virus integration.
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Title: Raltegravir, elvitegravir, and metoogravir: the birth of 'me-too' HIV-1 integrase inhibitors.
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Title: Characterization and structural analysis of HIV-1 integrase conservation.
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Title: Genetic barriers for integrase inhibitor drug resistance in HIV type-1 B and CRF02_AG subtypes.
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Title: Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection.
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Title: Clade-specific HIV-1 integrase polymorphisms do not reduce raltegravir and elvitegravir phenotypic susceptibility.
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Title: Genetic diversity of integrase (IN) sequences in antiretroviral treatment-naive and treatment-experienced HIV type 2 patients.
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