Dolutegravir interactions with HIV-1 integrase-DNA: structural rationale for drug resistance and dissociation kinetics. [PDF]
PLoS ONE, 2013 Signature HIV-1 integrase mutations associated with clinical raltegravir resistance involve 1 of 3 primary genetic pathways, Y143C/R, Q148H/K/R and N155H, the latter 2 of which confer cross-resistance to elvitegravir. In accord with clinical findings, in
Felix DeAnda +6 more
doaj +1 more source
AIDS (London), 2020 OBJECTIVE Excessive weight gain has been reported with integrase strand transfer inhibitors (INSTIs). We evaluated weight changes in virologically-suppressed adults with HIV who switched from non-INSTI regimens to raltegravir- or dolutegravir-containing ...
J. E. Burns +11 more
semanticscholar +1 more source
Weight gain among treatment-naïve persons with HIV starting integrase inhibitors compared to non-nucleoside reverse transcriptase inhibitors or protease inhibitors in a large observational cohort in the United States and Canada. [PDF]
, 2020 IntroductionWeight gain following antiretroviral therapy (ART) initiation is common, potentially predisposing some persons with HIV (PWH) to cardio-metabolic disease.
Altoff, Keri N +23 more
core +1 more source
Cryo-EM structure of the Rous sarcoma virus octameric cleaved synaptic complex intasome
Communications Biology, 2021 Pandey, Bera, Shi et al. report the cryo-electron microscopy structure of the Rous sarcoma virus octameric intasome complex stabilized by a HIV-1 integrase strand transfer inhibitor.
Krishan K. Pandey +8 more
doaj +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
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
In silico identification of potential natural product inhibitors of human proteases key to SARS-CoV-2 infection [PDF]
Molecules 2020, 25(17), 3822, 2020 Presently, there are no approved drugs or vaccines to treat COVID-19 which has spread to over 200 countries and is responsible for over 3,65,000 deaths worldwide. Recent studies have shown that two human proteases, TMPRSS2 and cathepsin L, play a key role in host cell entry of SARS-CoV-2.
arxiv +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