Patterns of resistance development with integrase inhibitors in HIV
Infection and Drug Resistance, 2011 Raltegravir, the only integrase (IN) inhibitor approved for use in HIV therapy, has recently been licensed. Raltegravir inhibits HIV-1 replication by blocking the IN strand transfer reaction. More than 30 mutations have been associated with resistance to raltegravir and other IN strand transfer inhibitors (INSTIs).
P Cane, Jean L. Mbisa, Martín
openalex +5 more sources
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
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
Microorganisms, 2021 Background: HIV infects around one hundred thousand patients in the Republic of the Congo. Approximately 25% of them receive an antiretroviral treatment; current first-line regimens include two NRTIs and one NNRTI, reverse transcriptase inhibitors ...
Ferdinand Emaniel Brel Got +7 more
doaj +1 more source
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
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
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
Allosteric HIV-1 integrase inhibitors lead to premature degradation of the viral RNA genome and integrase in target cells [PDF]
, 2017 Recent evidence indicates that inhibition of HIV-1 integrase (IN) binding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through mutations within IN yields aberrant particles in which the viral ribonucleoprotein complexes (vRNPs)
Elliott, Jennifer +8 more
core +2 more sources