integrase strand transfer inhibitor
Characterization of the R263K Mutation in HIV-1 Integrase That Confers Low-Level Resistance to the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir
... HIV-1 integrase, the R263K mutation was introduced by site-directed mutagenesis into the coding sequence of the subtype B integrase carrying the solubility mutations F185H and ...recombinant ...
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The Combination of the R263K and T66I Resistance Substitutions in HIV-1 Integrase Is Incompatible with High-Level Viral Replication and the Development of High-Level Drug Resistance
... in integrase has been selected in tissue culture with dolutegravir (DTG) and has been reported for sev- eral treatment-experienced individuals receiving DTG as part of salvage ...different integrase ...
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Switch rates, time to switch, and switch patterns of antiretroviral therapy in people living with human immunodeficiency virus in Japan, in a hospital claim database
... transcriptase inhibitor, PI: protease inhibitor, INSTI: integrase strand transfer inhibitor, ABC: abacavir, TDF: tenofovir disoproxil fumarate, 3TC: lamivudine, FTC: ...entry ...
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Clinical effectiveness of dolutegravir in the treatment of HIV/AIDS
... second-generation integrase strand transfer inhibitor (INSTI), which has now been licensed to be used in different countries including the ...
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Raltegravir for HIV-1 infected children and adolescents: efficacy, safety, and pharmacokinetics
... HIV integrase strand-transfer inhibitor to be approved by the US FDA, in October 2007, for the treatment of HIV-1 infection in combination with other antiretroviral ...
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Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors
... first-in-class inhibitor raltegravir (RAL) was licensed in 2007 ...DNA strand transfer activity, the drugs are referred to as IN strand transfer inhibitors (INSTIs) ...
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Altered Viral Fitness and Drug Susceptibility in HIV-1 Carrying Mutations That Confer Resistance to Nonnucleoside Reverse Transcriptase and Integrase Strand Transfer Inhibitors
... suspended in 50 l of medium were added to each well; the final volume in each well was 200 l. After incubation at 37°C for 48 h,  -galactosidase activity was quantified using a Galacto-Light Plus  -galactosidase ...
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Viral fitness cost prevents HIV 1 from evading dolutegravir drug pressure
... that integrase strand transfer inhibitors can be used to treat HIV-1 ...first-generation integrase inhibitors are susceptible to the emergence of resistance mutations that impair their ...
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In vitro activity of dolutegravir against wild type and integrase inhibitor resistant HIV 2
... that integrase strand transfer inhibitors (INSTI) might be particularly useful for HIV-2 ...at integrase residues Y143, Q148 or N155, together with other secondary replacements in the ...
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In Silicodocking of HIV 1 integrase inhibitors reveals a novel drug type acting on an enzyme/DNA reaction intermediate
... Results: Structural superimpositions suggested that a two-metal model for HIV-1 IN CCD in complex with small molecule, 1-(5-chloroindol-3-yl)-3-(tetrazoyl)-1,3-propandione-ene (5CITEP) could be used as a surrogate for an ...
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AN IN SILICO APPROACH TO IDENTIFY NEW ANTI HIV INTEGRASE INHIBITOR LIKE LEADS BY DOCKING STUDIES
... HIV-1 integrase (IN) has a crucial role to catalyzes the integration between viral DNA to host DNA Strand, this process important for virus replication cycle 4 , because human itself no such type of ...
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Mutations Located outside the Integrase Gene Can Confer Resistance to HIV 1 Integrase Strand Transfer Inhibitors
... Phenotypic analysis. Single-cycle titers of the virus were determined in HeLa P4 cells in which the expression of  -galactosidase was induced by the HIV Tat protein and quantified 48 h postinfection with chlorophenol red ...
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Efficient initiation and strand transfer of polypurine tract-primed plus-strand DNA prevent strand transfer of internally initiated plus-strand DNA.
... Southern analyses of DNAs from all three pools of cells gave similar results. A representative example of the Southern blots is shown in Fig. 5B. The expected 2.8- and 1.85-kb bands were observed in DNA samples digested ...
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Repair of Gaps in Retroviral DNA Integration Intermediates
... gaps. Integrase binds stably to the viral cDNA ends in PICs (10, 35, 51), suggesting that integrase may remain bound to integration products as ...for integrase to be actively removed from ...
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Human immunodeficiency virus integrase inhibitors efficiently suppress feline immunodeficiency virus replication in vitroand provide a rationale to redesign antiretroviral treatment for feline AIDS
... Starting with conservation of important HIV-1 and FIV IN residues, we built a 3D model of IN CCD of the Petaluma strain of FIV (FIV-Pet) by homology with HIV-1 IN CCD. Homology modeling of FIV IN CCD based on a crystal ...
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HIV Drug Resistance: An Overview
... an inhibitor of HIV- RT. This inhibitor has stimulated considerable interest as it appears to inhibit many strains of nucleoside analogue resistant HIV-1 (3, ...
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Progress in development of HIV 1 integrase inhibitor
... third strand that binds in the major groove to form base ...triplex inhibitor is the oligonucleotide designed to bind duplex DNA (or RNA) by a third nucleic acid strand to form a triple ...the ...
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Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS
... early stages of drug development for HIV-1, most of the drugs were targeted against HIV-1 reverse transcriptase and protease. However, life-long administration of drugs required to contain viral replication to a minimum ...
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Raltegravir in treatment naïve patients
... first integrase inhibitor to be ap- proved for the use in the treatment of HIV ...an integrase inhibitor, suggesting a reduced second phase decline of HIV-RNA in patients treated with this ...
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Rous sarcoma virus integrase protein: mapping functions for catalysis and substrate binding.
... Purified mutant proteins and wild-type RSV integrase were analyzed for their relative activities in vitro on oligonucleotide substrates designed to monitor terminal cleavage, strand tran[r] ...
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