Results 1 to 10 of about 19,019 (189)

Allosteric Integrase Inhibitor Influences on HIV-1 Integration and Roles of LEDGF/p75 and HDGFL2 Host Factors [PDF]

Viruses, 2022
Allosteric integrase (IN) inhibitors (ALLINIs), which are promising preclinical compounds that engage the lens epithelium-derived growth factor (LEDGF)/p75 binding site on IN, can inhibit different aspects of human immunodeficiency virus 1 (HIV-1 ...
Parmit Kumar Singh, Wen Li, Gregory J. Bedwell, Hind J. Fadel, Eric M. Poeschla, Alan N. Engelman   +5 more
doaj   +2 more sources

The structural and mechanistic bases for the viral resistance to allosteric HIV-1 integrase inhibitor pirmitegravir [PDF]

mBio
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are investigational antiretroviral agents that potently impair virion maturation by inducing hyper-multimerization of IN and inhibiting its interaction with viral genomic RNA. The pyrrolopyridine-based
Tung Dinh, Zahira Tber, Juan S. Rey, Seema Mengshetti, Arun S. Annamalai, Reed Haney, Lorenzo Briganti, Franck Amblard, James R. Fuchs, Peter Cherepanov, Kyungjin Kim, Raymond F. Schinazi, Juan R. Perilla, Baek Kim, Mamuka Kvaratskhelia   +14 more
doaj   +3 more sources

Pre-Treatment Integrase Inhibitor Resistance and Natural Polymorphisms among HIV-1 Subtype C Infected Patients in Ethiopia [PDF]

Viruses, 2022
Dolutegravir-based antiretroviral therapy (ART) has been scaled up in many developing countries, including Ethiopia. However, subtype-dependent polymorphic differences might influence the occurrence of HIV-drug-resistance mutations (HIVDRMs). We analyzed
Dawit Assefa Arimide, Zsófia Ilona Szojka, Kidist Zealiyas, Atsbeha Gebreegziabxier, Fekadu Adugna, Sviataslau Sasinovich, Per Björkman, Patrik Medstrand   +7 more
doaj   +2 more sources

Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis. [PDF]

PLoS ONE, 2013
BACKGROUND: Optimal regimen choice of antiretroviral therapy is essential to achieve long-term clinical success. Integrase inhibitors have swiftly been adopted as part of current antiretroviral regimens.
Peter Messiaen, Annemarie M J Wensing, Axel Fun, Monique Nijhuis, Nele Brusselaers, Linos Vandekerckhove   +5 more
doaj   +1 more source

Structural Studies of the HIV-1 Integrase Protein: Compound Screening and Characterization of a DNA-Binding Inhibitor. [PDF]

PLoS ONE, 2015
Understanding the HIV integrase protein and mechanisms of resistance to HIV integrase inhibitors is complicated by the lack of a full length HIV integrase crystal structure. Moreover, a lentiviral integrase structure with co-crystallised DNA has not been
Peter K Quashie, Ying-Shan Han, Said Hassounah, Thibault Mesplède, Mark A Wainberg   +4 more
doaj   +1 more source

Structural and functional role of INI1 and LEDGF in the HIV-1 preintegration complex. [PDF]

PLoS ONE, 2013
Integration of the HIV-1 cDNA into the human genome is catalyzed by the viral integrase (IN) protein. Several studies have shown the importance of cellular cofactors that interact with integrase and affect viral integration and infectivity. In this study,
Benoit Maillot, Nicolas Lévy, Sylvia Eiler, Corinne Crucifix, Florence Granger, Ludovic Richert, Pascal Didier, Julien Godet, Karine Pradeau-Aubreton, Stéphane Emiliani, Alexis Nazabal, Paul Lesbats, Vincent Parissi, Yves Mely, Dino Moras, Patrick Schultz, Marc Ruff   +16 more
doaj   +1 more source

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, Kendra E Hightower, Robert T Nolte, Kazunari Hattori, Tomokazu Yoshinaga, Takashi Kawasuji, Mark R Underwood   +6 more
doaj   +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, Sibes Bera, Ke Shi, Michael J. Rau, Amarachi V. Oleru, James A. J. Fitzpatrick, Alan N. Engelman, Hideki Aihara, Duane P. Grandgenett   +8 more
doaj   +1 more source

HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure

Retrovirology, 2009
In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin, Deris Zaquan, Herring Belinda, van Hal Sebastiaan J, Saksena Nitin K, Dwyer Dominic E   +5 more
doaj   +1 more source

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, Dana N Raugi, Charlotte Pan, Matthew Coyne, Alexandra Hernandez, Brad Church, Kara Parker, James I Mullins, Papa Salif Sow, Geoffrey S Gottlieb, University of Washington-Dakar HIV-2 Study Group   +10 more
doaj   +1 more source