Multimodal Functionalities of HIV-1 Integrase
Viruses, 2022 Integrase is the retroviral protein responsible for integrating reverse transcripts into cellular genomes. Co-packaged with viral RNA and reverse transcriptase into capsid-encased viral cores, human immunodeficiency virus 1 (HIV-1) integrase has long ...
Alan N. Engelman, Mamuka Kvaratskhelia
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Novel therapeutic strategies targeting HIV integrase [PDF]
BMC Medicine, 2012 Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an ...
Quashie Peter K +2 more
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Arylamide Inhibitors of HIV-1 Integrase
Journal of Medicinal Chemistry, 1997 Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency.
He Zhao +5 more
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Incorporation of aptamers in the terminal loop of shRNAs yields an effective and novel combinatorial targeting strategy. [PDF]
, 2017 Gene therapy by engineering patient's own blood cells to confer HIV resistance can potentially lead to a functional cure for AIDS. Toward this goal, we have previously developed an anti-HIV lentivirus vector that deploys a combination of shRNA, ribozyme ...
Castanotto, Daniela +4 more
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Authentic HIV-1 Integrase Inhibitors [PDF]
Future Medicinal Chemistry, 2010 HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Chenzhong, Liao +4 more
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Drug resistance in B and non-B subtypes amongst subjects recently diagnosed as primary/recent or chronic HIV-infected over the period 2013–2016: Impact on susceptibility to first-line strategies including integrase strand-transfer inhibitors [PDF]
, 2017 Objectives To characterize the prevalence of transmitted drug resistance mutations (TDRMs) by plasma analysis of 750 patients at the time of HIV diagnosis from January 1, 2013 to November 16, 2016 in the Veneto region (Italy), where all drugs included in
Alvarez, M +18 more
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Treatment of HIV Infections with HIV Integrase Inhibitors. [PDF]
ACS Med Chem Lett, 2017 Abdel-Magid AF.
europepmc +4 more sources
Resistance to inhibitors of the human immunodeficiency virus type 1 integration
Brazilian Journal of Infectious Diseases, 2010 This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Daria J. Hazuda, PhD
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Dialysis purification of integrase-DNA complexes provides high-resolution atomic force microscopy images: dimeric recombinant HIV-1 integrase binding and specific looping on DNA. [PDF]
PLoS ONE, 2013 It remains difficult to obtain high-resolution atomic force microscopy images of HIV-1 integrase bound to DNA in a dimeric or tetrameric fashion. We therefore constructed specific target DNAs to assess HIV-1 integrase binding and purified the complex by ...
Tatsuaki Tsuruyama +5 more
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Protein expression from unintegrated HIV-1 DNA introduces bias in primary in vitro post-integration latency models [PDF]
, 2016 To understand the persistence of latently HIV-1 infected cells in virally suppressed infected patients, a number of in vitro models of HIV latency have been developed.
Bonczkowski, Pawel +7 more
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