[PDF] Top 20 Patterns of resistance development with integrase inhibitors in HIV
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Patterns of resistance development with integrase inhibitors in HIV
... drug-resistant HIV-1 variants in patients undergoing HAART remains a major reason for treatment failure in HIV-1 ...fusion inhibitors, entry inhibitors, and integrase (IN) ...of ... See full document
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HIV Integrase Inhibitors Block Replication of Alpha , Beta , and Gammaherpesviruses
... different patterns of sensitivity, so each will need to be screened with this and other panels of ...from HIV in- tegrase inhibitor screens could be sources of additional com- pounds that have anti-herpes ... See full document
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Allosteric HIV-1 Integrase Inhibitors Lead to Premature Degradation of the Viral RNA Genome and Integrase in Target Cells
... mutant virus was markedly resistant to BI-B2 (Fig. 1A). As expected, BI-B2 treatment did not affect the binding of virions to cells, as similar levels of CA (Fig. 1B), IN (Fig. 1B), and vRNA (Fig. 1C) were present ... See full document
22
HIV drug resistance against strand transfer integrase inhibitors
... INSTI resistance may be important, as the GGA glycine codon can more easily transition to AGA, explaining why arginine is present at a higher frequency in non-B subtypes ...secondary resistance mutations ... See full document
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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
... tance patterns and mechanisms of EVG, the HIV-1 IIIB strains selected in the presence of increasing concentrations of this IN inhibitor were analyzed genotypically and phenotypi- cally at different stages ... See full document
9
Limited Marginal Utility of Deep Sequencing for HIV Drug Resistance Testing in the Age of Integrase Inhibitors
... for HIV drug resistance detection is also complicated by the ever-changing landscape of HIV ...of HIV-1 resistance mutations associated with nonnucleoside reverse transcriptase ... See full document
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Mutations Located outside the Integrase Gene Can Confer Resistance to HIV 1 Integrase Strand Transfer Inhibitors
... the resistance to ...nef-defective HIV-1 show strongly attenuated viral replication and pathogenesis ...the resistance of the virus to DTG and ...in resistance to DTG when associated with ... See full document
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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
... drug resistance mutations associated with NRTIs (K65R) (16) and InSTI (M154I) (12) in M4 after rebound and M5 at failure (Table ...raltegravir resistance (E92Q) ...of integrase in relation to drug ... See full document
5
Prevalence of resistance to integrase strand transfer inhibitors (INSTIs) among untreated HIV 1 infected patients in Morocco
... drug resistance according to the Stanford algorithm. Sixty samples were HIV-1 subtype B (78%), fourteen CRF02_AG (18%), two subtype C and one subtype ...INSTIs resistance mutation were absent, ... See full document
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Molecular Modeling of Potential Dual Inhibitors of HIV Reverse Transcriptase and Integrase
... with HIV-1 ...fusion inhibitors, reverse transcriptase (RT) inhibitors (that include nucleoside, NRTIs and nonnucleo- side, NNRTIs), integrase (IN), and protease (PI) inhibitors ...IN ... See full document
41
Dual Selection Pressure by Drugs and HLA Class I-Restricted Immune Responses on Human Immunodeficiency Virus Type 1 Protease
... the development of resistance mutations, we focused on the B44-restricted epitope EW9 (EEMNLPGRW; PR amino acids 34 to 42) (33) and the A2-restricted epitope KI10 (KMIGGI GGFI; PR amino acids 45 to 54) ... See full document
12
Raltegravir in the management of HIV-infected patients
... other integrase inhibitors in development (Goethals et al ...mutated integrase enzymes displayed an impairment of enzyme function (Malet et al 2008), indicating reduced replicative fi ...in ... See full document
8
Progress in development of HIV 1 integrase inhibitor
... is HIV-1 ...enzyme integrase, is a pivotal step in viral life cycle and thus worthy of being exploited to develop anti-HIV ...the HIV-1 integrase to develop anti-HIV ... See full document
15
Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection
... and integrase genotype data were available for 60 ...and resistance mutations suggests a rela- tively low genetic barrier for the development of resistance if viral suppression is not ... See full document
10
HIV 1 integrase inhibitors are substrates for the multidrug transporter MDR1 P glycoprotein
... gp inhibitors such as verapamil during incubation and/or drug extrusion, restores doxorubicin ...VBL resistance profile indicat- ing a significant inhibition of P-gp ... See full document
10
Raltegravir, elvitegravir, and metoogravir: the birth of "me too" HIV 1 integrase inhibitors
... drug resistance most often results from the substitution of one of three amino acids – Y143, Q148, or N155 – usually in combination with at least one other mutation ...viral resistance to raltegravir ... See full document
14
Inhibitors of the integrase–transportin SR2 interaction block HIV nuclear import
... three HIV enzymes to be targeted by cART. To date, three IN inhibitors have been approved for clinical use (raltegravir, elvitegravir and dolutegravir), all belonging to a class of catalytic site ... See full document
13
Characterization of a Replication-Competent, Integrase-Defective Human Immunodeficiency Virus (HIV)/Simian Virus 40 Chimera as a Powerful Tool for the Discovery and Validation of HIV Integrase Inhibitors
... defining integrase (IN) as a target for anti- retroviral ...IN inhibitors, and a variety of chemical classes have been ...inhibits HIV-1 replication and IN activity in vitro (22) yet primarily blocks ... See full document
5
Resistance to the Anti-Human Immunodeficiency Virus Type 1 Compound l-Chicoric Acid Results from a Single Mutation at Amino Acid 140 of Integrase
... of HIV integration within the cell has proven difficult to ...drug resistance maps to changes in the amino acid sequence of a viral ...of HIV to nucleoside and nonnucleoside RT inhibitors maps ... See full document
5
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, ... See full document
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