Hiv 1 integrase
![Synthesis, antiinflammatory and HIV-1 integrase inhibitory activities of 1,2-bis[5-thiazolyl]ethane-1,2-dione derivatives](data:image/gif;base64,R0lGODlhAQABAIAAAP///wAAACH5BAEAAAAALAAAAAABAAEAAAICRAEAOw==)
Synthesis, antiinflammatory and HIV-1 integrase inhibitory activities of 1,2-bis[5-thiazolyl]ethane-1,2-dione derivatives
... the integrase assay few compounds showed weak activity (Table ...potent HIV-1 integrase inhibitors, besides the diketo moiety an additional carboxylic acid moiety is present and this feature ...
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Uneven Genetic Robustness of HIV-1 Integrase
... like HIV-1 that exhibit high mutation rates and exist in immu- nologically hostile ...the HIV-1 capsid protein (CA) exhibits extreme ...of HIV-1 proteins, we created a large ...
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Histone deacetylase 1 interacts with HIV 1 Integrase and modulates viral replication
... the HIV integrase, we have developed a purification method based on the use of streptavidin magnetic beads coupled to the integrase and the viral DNA of ...that HIV-1 integrase ...
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Progress in development of HIV 1 integrase inhibitor
... enzyme integrase, is a pivotal step in viral life cycle and thus worthy of being exploited to develop anti-HIV ...chemotherapy. HIV-1 integrase is comprised of three domains (Figure II) ...
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CURRENT STATUS OF HIV-1 INTEGRASE INHIBITORS
... type 1 (HIV-1), remains a serious global health ...of HIV-resistant strains, and the long-term goal of eradicating the virus from infected cells is still ...is HIV-1 ...
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Allosteric HIV-1 Integrase Inhibitors Lead to Premature Degradation of the Viral RNA Genome and Integrase in Target Cells
... of 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 ...
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HIV 1 integrase inhibitors are substrates for the multidrug transporter MDR1 P glycoprotein
... of HIV-1 Integrase (IN) (IN inhibitors, IINs) has played a major role in validating this enzyme as an important target for antiretroviral ...where HIV-1 replicates, we determined ...
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Raltegravir, elvitegravir, and metoogravir: the birth of "me too" HIV 1 integrase inhibitors
... (Table 1) ...(Table 1) [67,71-73], we next used our docking technique to attempt to effectively predict these interactions (Figure ...selected HIV-1 integrase inhibitors upon ...
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HIV 1 integrase modulates the interaction of the HIV 1 cellular cofactor LEDGF/p75 with chromatin
... Myc-tagged HIV-1 integrase was detected with anti-Myc Mab (1/500, clone 9E10, Covance) and alpha tubulin was detected as a loading control with anti-alpha tubulin Mab (1/4000, Clone ...
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Effect of HIV-1 Integrase Resistance Mutations When Introduced into SIVmac239 on Susceptibility to Integrase Strand Transfer Inhibitors
... for HIV-1 that showed that DTG was active against most RAL- and EVG-resistant viruses that contained only one or two INSTI mutations (25, 52), as well as with results that both R263K and G118R can be ...
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Inhibition of HIV 1 integrase nuclear import and replication by a peptide bearing integrase putative nuclear localization signal
... An interaction between HIV-1 IN and importin α was first demonstrated by Gallay et al. [8]. Similarly an interaction between the IN and members of the importin family and that its nuclear transport appears ...
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Mutations Located outside the Integrase Gene Can Confer Resistance to HIV 1 Integrase Strand Transfer Inhibitors
... Alamos HIV-1 database, representing a total of 23,874 sequences, showed that the motif was highly conserved, with each G considered individually showing variability on the order of ...
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Importin α3 Interacts with HIV-1 Integrase and Contributes to HIV-1 Nuclear Import and Replication
... during HIV nuclear import (1, 2, 6, 10, 16, 20), we first used an in vitro pulldown assay to test for an interaction between HIV IN and Imp ␣ ...whether HIV IN could bind directly to Imp ␣ 3 ...
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Characterization of the HIV 1 integrase chromatin and LEDGF/p75 binding abilities by mutagenic analysis within the catalytic core domain of integrase
... Because LEDGF/p75 has been shown to be involved in IN chromatin targeting, we also tested the LEDGF/p75- binding ability of different IN mutants by a cell-based co-IP assay. Equal amounts of T7-LEDGF and CMV- YFP-IN ...
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Peptides derived from the HIV 1 integrase promote HIV 1 infection and multi integration of viral cDNA in LEDGF/p75 knockdown cells
... interaction with the Rev protein [14,17,18,22]. It is pos- sible, however, that the few integration events that do occur in virus-infected cells are mediated by IN mole- cules which were translocated, as IN-DNA ...
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GCN5 dependent acetylation of HIV 1 integrase enhances viral integration
... To confirm the in vitro observation that IN is a substrate for both GCN5 and p300, an antibody specific to acety- lated IN was produced by using an IN-derived peptide for immunization. The IN-derived peptide was chemi- ...
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Efficacies of Cabotegravir and Bictegravir against drug resistant HIV 1 integrase mutants
... Based on these results, BIC appears to be a very prom- ising INSTI. CAB has obvious disadvantages in terms of its breadth of antiviral potency relative to both BIC and DTG. However, CAB may have other advantages; it can ...
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Changes in the accessibility of the HIV 1 Integrase C terminus in the presence of cellular proteins
... the integrase was C-terminally tagged with an HA epitope (IN-HAv) (see Materials and ...the integrase was efficiently immunoprecipitated with an anti-HA antibody from the lysed IN-HAv, but was poorly pulled ...
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Integrase and integration: biochemical activities of HIV 1 integrase
... the integrase oligomer and viral DNA molecule form part of a preintegration complex (PIC), our knowl- edge of which remains ...intact integrase is required for the stabilisation of preintegration complexes ...
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Molecular evolution of HIV 1 integrase during the 20 years prior to the first approval of integrase inhibitors
... in HIV evolution is debated and has been quantified to some extent at the level of intra-patient evolution and for known transmission pairs rather than on inter-patient level [60, ...the integrase may be ...
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