Results 21 to 30 of about 2,808,349 (298)

Resistance to Integrase Inhibitors [PDF]

Viruses, 2010
Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance.
Yves Pommier, Kasthuraiah Maddali, Mathieu Métifiot, Christophe Marchand   +3 more
openaire   +4 more sources

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 basis of second-generation HIV integrase inhibitor action and viral resistance

Science, 2020
Strengths and weaknesses of an HIV drug Retroviruses replicate by inserting a copy of their RNA, which has been reverse transcribed into DNA, into the host genome. This process involves the intasome, a nucleoprotein complex comprising copies of the viral
N. Cook, Wen Li, D. Berta, M. Badaoui, A. Ballandras-Colas, A. Nans, A. Kotecha, E. Rosta, A. Engelman, P. Cherepanov   +9 more
semanticscholar   +1 more source

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

Viruses, 2021
There are limited real-world mutational and virological outcomes data of treatment-experienced persons diagnosed with HIV-1 subtype C (HIV-1 C) who are failing Integrase Strand Transfer Inhibitor-based regimens. Requisition forms sent for HIV-1 genotypic
K. Seatla, D. Maruapula, W. Choga, Tshenolo Ntsipe, Nametso Mathiba, Mompati L Mogwele, Max Kapanda, B. Nkomo, Dinah Ramaabya, J. Makhema, M. Mmalane, M. Mine, I. Kasvosve, S. Lockman, S. Moyo, S. Gaseitsiwe   +15 more
semanticscholar   +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

Mutations in the HIV-1 3′-Polypurine Tract and Integrase Strand Transfer Inhibitor Resistance

Antimicrobial Agents and Chemotherapy, 2021
Integrase strand-transfer inhibitors (INSTIs), in combination with other antivirals, are widely used for the treatment of HIV-1-infected individuals. HIV-1 resistance to INSTIs is typically associated with mutations in the viral integrase gene [1].….
Yuliang Wei, N. Sluis-Cremer
semanticscholar   +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

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, Bourgi, Kassem, Crane, Heidi, Gange, Stephen J, Gill, John, Horberg, Michael A, Jenkins, Cathy A, Kirk, Gregory, Koethe, John R, Lake, Jordan, Li, Jun, Lima, Viviane D, Margolick, Joseph, Mathews, William C, Moore, Richard D, North American AIDS Cohort Collaboration on Research and Design (NA-ACCORD), Palella, Frank, Rabkin, Charles S, Rebeiro, Peter F, Silverberg, Michael, Sterling, Timothy R, Thorne, Jennifer, Willig, Amanda, Wong, Cherise   +23 more
core   +1 more source

No overall change in the rate of weight gain after switching to an integrase-inhibitor in virologically suppressed adults with HIV.

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, Oliver T. Stirrup, D. Dunn, Iain Runcie-Unger, A. Milinkovic, S. Candfield, Hinal Lukha, Abigail Severn, L. Waters, S. Edwards, R. Gilson, S. Pett   +11 more
semanticscholar   +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