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
openalex +3 more sources
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
core +3 more sources
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
doaj +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
core +1 more source
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
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
Switching from a protease inhibitor-based regimen to a dolutegravir-based regimen : a randomized clinical trial to determine the effect on peripheral blood and ileum biopsies from antiretroviral therapy-suppressed human immunodeficiency virus-infected individuals [PDF]
, 2018 Background: Optimization of combination antiretroviral therapy (cART) can impact the human immunodeficiency virus (HIV) reservoir. We evaluated the effect on the HIV reservoir in peripheral blood and ileum biopsies in patients switching from boosted ...
Blanco, Julià +15 more
core +3 more sources
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
Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes
Retrovirology, 2009 Background Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes ...
Kuhl Björn D +7 more
doaj +1 more source