Results 11 to 20 of about 14,793 (172)

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, Donahue Daniel A, Faltenbacher Verena H, Sloan Richard D, Bar-Magen Tamara, Oliveira Maureen, Xu Hongtao, Wainberg Mark A   +7 more
doaj   +1 more source

Emergence of the G118R Pan-Integrase Resistance Mutation as a Result of Low Compliance to a Dolutegravir-Based cART

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, Lasse Fjordside, Jannik Fonager, Jan Gerstoft   +3 more
doaj   +1 more source

Absence of Resistance Mutations in the Integrase Coding Region among ART-Experienced Patients in the Republic of the Congo

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, Patricia Recordon-Pinson, Ghislain Loubano-Voumbi, Dagene Ebourombi, Marie-Lise Blondot, Mathieu Metifiot, Gontran Ondzotto, Marie-Line Andreola   +7 more
doaj   +1 more source

Novel therapeutic strategies targeting HIV integrase

BMC Medicine, 2012
Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an ...
Quashie Peter K, Sloan Richard D, Wainberg Mark A   +2 more
doaj   +1 more source

CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones

E-Journal of Chemistry, 2010
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
doaj   +1 more source

Mutations Located outside the Integrase Gene Can Confer Resistance to HIV-1 Integrase Strand Transfer Inhibitors

mBio, 2017
Resistance to the integrase strand transfer inhibitors raltegravir and elvitegravir is often due to well-identified mutations in the integrase gene. However, the situation is less clear for patients who fail dolutegravir treatment.
Isabelle Malet, Frédéric Subra, Charlotte Charpentier, Gilles Collin, Diane Descamps, Vincent Calvez, Anne-Geneviève Marcelin, Olivier Delelis   +7 more
doaj   +1 more source

Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence

Viruses, 2015
Drug resistance prevents the successful treatment of HIV-positive individuals by decreasing viral sensitivity to a drug or a class of drugs. In addition to transmitted resistant viruses, treatment-naïve individuals can be confronted with the problem of ...
Thibault Mesplède, Mark A. Wainberg
doaj   +1 more source

Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors

Viruses, 2010
The HIV-1 integrase enzyme is essential for integrating the viral DNA into the host chromosome. Infection is aborted in the absence of integration, making integrase an attractive antiviral target. Recently approved inhibitors of integrase bind tightly to
Robert Craigie, Zhiqi Yin
doaj   +1 more source

The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function

mBio, 2023
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer, Tung Dinh, Lev Levintov, Arun S. Annamalai, Juan S. Rey, Lorenzo Briganti, Nicola J. Cook, Valerie E. Pye, Ian A. Taylor, Kyungjin Kim, Alan N. Engelman, Baek Kim, Juan R. Perilla, Mamuka Kvaratskhelia, Peter Cherepanov   +14 more
doaj   +1 more source

Molecular features related to HIV integrase inhibition obtained from structure- and ligand-based approaches. [PDF]

PLoS ONE, 2014
Among several biological targets to treat AIDS, HIV integrase is a promising enzyme that can be employed to develop new anti-HIV agents. The aim of this work is to propose a mechanistic interpretation of HIV-1 integrase inhibition and to rationalize the ...
Luciana L de Carvalho, Vinícius G Maltarollo, Emmanuela Ferreira de Lima, Karen C Weber, Kathia M Honorio, Albérico B F da Silva   +5 more
doaj   +1 more source