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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Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design. [PDF]
PLoS ONE, 2012 A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived growth factor (LEDGF) binding site of the integrase catalytic core domain.
Thomas S Peat +15 more
doaj +1 more source
INSTIs and NNRTIs Potently Inhibit HIV-1 Polypurine Tract Mutants in a Single Round Infection Assay
Viruses, 2021 Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral compounds that prevent the insertion of a DNA copy of the viral genome into the host genome by targeting the viral enzyme integrase (IN).
Steven J. Smith +6 more
doaj +1 more source
Infectious Disease Reports, 2022 HIV-1 resistance towards integrase inhibitors is a potential threat of the success of HIV-1 combination treatment. G118R is a rare drug resistance mutation conferring pan-integrase resistance.
Helene Mens +3 more
doaj +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
Prevalence of resistance mutations associated with integrase inhibitors in therapy-naive HIV-positive patients in Hungary [PDF]
, 2021 Widespread introduction of HIV integrase inhibitors into clinical care may result in appearance of drug resistance mutations affecting treatment outcome.
Lakatos Botond +5 more
core +1 more source
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.
Terrence R. Burke +4 more
openaire +3 more sources
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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Adaptive HIV-1 evolutionary trajectories are constrained by protein stability [PDF]
, 2017 Despite the use of combination antiretroviral drugs for the treatment of HIV-1 infection, the emergence of drug resistance remains a problem. Resistance may be conferred either by a single mutation or a concerted set of mutations.
Kandathil, Shaun M. +3 more
core +1 more source