integrase inhibitors
HIV Integrase Inhibitors Block Replication of Alpha , Beta , and Gammaherpesviruses
... HIV integrase is contained within an RNase H-like fold, and numerous drugs have been devel- oped that bind to this site and inhibit its ...HIV integrase inhibitors might also inhibit HSV replication ...
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HIV/HCV-coinfection: which role can new antiretrovirals such as integrase inhibitors play?
... the integrase inhibitors, raltegravir is currently the only licensed integrase inhibitor for the treatment of HIV-infection and has thus most clinical data avail- ...S/GSK1349572, integrase ...
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Allosteric HIV-1 Integrase Inhibitors Lead to Premature Degradation of the Viral RNA Genome and Integrase in Target Cells
... HIV-1 integrase (IN) binding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through muta- tions within IN yields aberrant particles in which the viral ribonucleoprotein com- ...
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Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection
... grase inhibitors, in addition to other new drugs that attack different targets such as entry and viral maturation, could possibly be used to create even more potent drug regimens that we use ...Although ...
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Lack of integrase inhibitors associated resistance mutations among HIV 1C isolates
... countries integrase strand transfer inhibitors have been shown to lead to virological sup- pression in both treatment naïve patient as well as treat- ment-experienced individuals with multidrug-resistance ...
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CURRENT STATUS OF HIV-1 INTEGRASE INHIBITORS
... of integrase inhibitors in the treatment of HIV and recent advances along current status of HIV 1 integrase ...HIV integrase (IN) is a target that has been the focus of rational drug design ...
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Raltegravir, elvitegravir, and metoogravir: the birth of "me too" HIV 1 integrase inhibitors
... . In clin- ical experimental resistance profiling, the V151I mutation has been observed to confer up to an 18-fold resistance to L870,810, while the same mutation had a negligible effect on viral resistance to ...
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Limited Marginal Utility of Deep Sequencing for HIV Drug Resistance Testing in the Age of Integrase Inhibitors
... Another limitation of our study is its low power. Despite significant efforts exerted to obtain a sufficiently large cohort size for the analysis, more than a third of patients in the test cohort were excluded from the ...
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Suppression of Human Immunodeficiency Virus Type 1 (HIV-1) Viremia with Reverse Transcriptase and Integrase Inhibitors, CD4+ T-Cell Recovery, and Viral Rebound upon Interruption of Therapy in a New Model for HIV Treatment in the Humanized Rag2−/−γc−/− Mouse
... In M5, following an initial decline, viremia increased rapidly. M4 exhibited a delayed response to ART. We sequenced the viral polymerase (pol) gene to seek evidence of drug resistance mutations. Amplicons were generated ...
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HIV drug resistance against strand transfer integrase inhibitors
... transfer inhibitors (INSTIs) are the newest class of antiretroviral drugs to be approved for treatment and act by inhibiting the essential HIV protein integrase from inserting the viral DNA genome into the ...
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The use of integrase inhibitors in treatment-experienced patients
... Raltegravir, the first approved HIV-1 integrase in- hibitor, is able to block the strand transfer step of the HIV proviral DNA integration process into the cellu- lar host DNA. The selected dosage for the pivotal ...
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HIV 1 integrase inhibitors are substrates for the multidrug transporter MDR1 P glycoprotein
... Doxorubucin is a fluorescent substrate for P-gp and incu- bation of P-gp-positive cells with this drug, followed by washing and further incubation at 37°C, results in a diminished fluorescence profile due to the active ...
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Resistance Mutations in Human Immunodeficiency Virus Type 1 Integrase Selected with Elvitegravir Confer Reduced Susceptibility to a Wide Range of Integrase Inhibitors
... To gain further understanding of the antiviral (cross-) resis- tance patterns and mechanisms of EVG, the HIV-1 IIIB strains selected in the presence of increasing concentrations of this IN inhibitor were analyzed ...
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Patterns of resistance development with integrase inhibitors in HIV
... Figure 1 HIv-1 DNA integration. HIv-1 virus synthesizes a dsDNA (red) copy of its RNA genome following entry of the virus into host cell cytoplasm. HIv-1 integrase removes 3′ end GT dinucleotides on both viral DNA ...
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In Silicodocking of HIV 1 integrase inhibitors reveals a novel drug type acting on an enzyme/DNA reaction intermediate
... In-silicodocking of integrase strand transfer inhibitors (INSTIs) at the integrase (IN) active site. The structure of INSTIs L-731,988 (Panel A), S-1360 (B), L-870,812 (C), L-870,810 (D), GS-9137 (E, ...
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Molecular evolution of HIV 1 integrase during the 20 years prior to the first approval of integrase inhibitors
... HIV-1 integrase polymorphisms and INSTI resistance mutations has been investigated before in INSTI-naïve individuals [26, 31–35] and ART-naïve individuals ...HIV-1 integrase sequences were obtained from ...
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Allosteric Integrase Inhibitors Reveal a Role for Integrase During HIV-1 Maturation
... IN inhibitors can inhibit recombinant IN nuclear transport in vitro (257) and reverse transcription and integration during HIV-1 infection (258), although the contributions of these different activities to ...
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Mutations Located outside the Integrase Gene Can Confer Resistance to HIV 1 Integrase Strand Transfer Inhibitors
... IMPORTANCE Integrase strand transfer inhibitors (INSTIs) are increasingly used both as first-line drugs and in rescue therapy because of their low toxicity and high effi- cacy in both treatment-naive and ...
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TALEN Knockout of the PSIP1 Gene in Human Cells: Analyses of HIV-1 Replication and Allosteric Integrase Inhibitor Mechanism
... lentiviral integrase proteins ...the integrase binding domain and plays no known virological ...Allosteric integrase inhibitors, or ALLINIs, also known as the noncatalytic site IN inhibitor ...
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Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors
... Integrase inhibitors are emerging anti-human immunodeficiency virus (HIV) drugs, and multiple retrovi- ruses and transposable elements were evaluated here for susceptibilities to raltegravir (RAL) and ...
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