Biochemical activity of RAGs is impeded by Dolutegravir, an HIV integrase inhibitor
Cell Death Discovery, 2020 HIV is a retrovirus that infects CD4 + T lymphocytes in human beings and causes immunodeficiency. In the recent years, various therapies have been developed against HIV, including targeting the HIV specific protein, integrase, responsible for integration
N. Nilavar +2 more
semanticscholar +1 more source
Journal of Antimicrobial Chemotherapy, 2020 Objectives HIV-1 integrase inhibitors are recommended as first-line therapy by WHO, though efficacy and resistance data for non-B subtypes are limited.
K. El Bouzidi +17 more
semanticscholar +1 more source
Investigation of furo[2,3-h]- and pyridazino[3,4-f]cinnolin-3-ol scaffolds as substrates for the development of novel HIV-1 integrase inhibitors [PDF]
, 2011 With the aim to develop novel HIV-1 integrase inhibitors, we obtained a set of condensed ring systems based on the furo[2,3-h]cinnolin-3(2H)-one and pyridazino[3,4-f]cinnolin-3-ol scaffolds bearing a potential chelating pharmacophore, which can be ...
Mohamed F. Y. Gomaa +7 more
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An Allosteric Mechanism for Inhibiting HIV-1 Integrase with a Small Molecule [PDF]
, 2009 HIV-1 integrase (IN) is a validated target for developing antiretroviral inhibitors. Using affinity acetylation and mass spectrometric (MS) analysis, we previously identified a tetra-acetylated inhibitor (2E)-3-[3,4-bis(acetoxy)phenyl]-2-propenoate-N ...
Burke, Terrence R., Jr. +7 more
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Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens. [PDF]
PLoS ONE, 2012 Human immunodeficiency virus type 2 (HIV-2) is intrinsically resistant to non-nucleoside reverse transcriptase inhibitors and exhibits reduced susceptibility to several of the protease inhibitors used for antiretroviral therapy of HIV-1. Thus, there is a
Robert A Smith +10 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
core +1 more source
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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Definitions, 2020 (75) Inventors: B. Narasimhulu Naidu, Durham, CT (US); Jacques Banville, St-Hubert (CA); Francis Beaulieu, Laprairie (CA); Timothy P. Connolly, Portland, CT (US); Mark R. Krystal, Westport, CT (US); John D. Matiskella, Wallingford, CT (US); Carl Ouellet,
J. Epperson
semanticscholar +1 more source
Nature Communications, 2019 Long-acting formulation of the integrase inhibitor cabotegravir (CAB LA) is in clinical development for HIV pre-exposure prophylaxis (PrEP). Here, using a SHIV macaque model, the authors show emergence of integrase mutations associated to CAB LA PrEP ...
Jessica Radzio-Basu +12 more
doaj +1 more source
Mathematical model of a serine integrase-controlled toggle switch with a single input [PDF]
, 2018 Dual-state genetic switches that can change their state in response to input signals can be used in synthetic biology to encode memory and control gene expression.
Colloms, Sean D. +3 more
core +1 more source