Results 21 to 30 of about 3,561 (181)

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

HIV-2 integrase variation in integrase inhibitor-naïve adults in Senegal, West Africa. [PDF]

PLoS ONE, 2011
Antiretroviral therapy for HIV-2 infection is hampered by intrinsic resistance to many of the drugs used to treat HIV-1. Limited studies suggest that the integrase inhibitors (INIs) raltegravir and elvitegravir have potent activity against HIV-2 in ...
Geoffrey S Gottlieb, Robert A Smith, Ndeye Mery Dia Badiane, Selly Ba, Stephen E Hawes, Macoumba Toure, Alison K Starling, Fatou Traore, Fatima Sall, Stephen L Cherne, Joshua Stern, Kim G Wong, Paul Lu, Moon Kim, Dana N Raugi, Airin Lam, James I Mullins, Nancy B Kiviat, Papa Salif Sow for the UW-Dakar HIV-2 Study Group   +18 more
doaj   +1 more source

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

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

Brazilian Journal of Infectious Diseases, 2010
This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection.
Daria J. Hazuda, PhD
doaj   +1 more source

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, David I Rhodes, Nick Vandegraaff, Giang Le, Jessica A Smith, Lisa J Clark, Eric D Jones, Jonathan A V Coates, Neeranat Thienthong, Janet Newman, Olan Dolezal, Roger Mulder, John H Ryan, G Paul Savage, Craig L Francis, John J Deadman   +15 more
doaj   +1 more source

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.
Szlávik János, Minárovits János, Lakatos Botond, Mezei Mária, Pocskay Ágnes, Áy Éva   +5 more
core   +3 more sources

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

Molecular monitoring of HIV-1 drug resistance in Ifakara HIV-1 Cohort, Tanzania [PDF]

, 2013
HIV-1 resistance is one of the problems affecting success of antiretroviral therapy programmes worldwide. Many studies on efficacy of ART programmes, specifically on drug resistance, have been conducted in developed countries but not in developing ...
Masimba, Pax Jessey
core   +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

5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors

, 2019
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for ...
Timothy Connolly (1754563), Dawn D. Parker (1834201), Christopher Cianci (6240926), Susan Jenkins (1834318), Kevin M. Peese (1457527), Barry L. Johnson (6240911), Robert T. Nolte (471200), Chen Li (54018), Hal A. Lewis (1399384), Christopher W. Allard (6240908), Brian McAuliffe (6240920), Nicholas A. Meanwell (362044), Manoj Patel (6240914), Mark Krystal (364355), Ping Zhang (86495), Michael A. Walker (1754566), Beatrice Minassian (6240923), Kevin Kish (1399378), Jean Simmermacher (5101232), Margaret E. Sorensen (6240917), B. Narasimhulu Naidu (2686801)   +20 more
core   +2 more sources