Results 11 to 20 of about 38,544 (277)

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

PLoS ONE, 2013
BackgroundOptimal 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. The purpose of this study was to review the evidence
Peter Messiaen, Annemarie M J Wensing, Axel Fun, Monique Nijhuis, Nele Brusselaers, Linos Vandekerckhove   +5 more
doaj   +10 more sources

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

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   +4 more sources

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

Real‐world use of second‐generation integrase strand transfer inhibitors ( INSTI ) as switch therapy in the prospective ANRS ‐ CO3 ‐ AquiVIH ‐ NA cohort

HIV Medicine, EarlyView.
Abstract Objectives To characterize real‐world treatment switching in France to bictegravir (BIC or B) or dolutegravir (DTG)‐based regimens with a focus on treatment persistence, effectiveness (HIV‐1 RNA ≤50 copies/ml) and particular attention to the prevalence and incidence of comorbidities. Methods People living with HIV from the prospective ANRS‐CO3‐
O. Leleux, A. Peyrouny‐Mazeau, A. Perrier, M. Hessamfar, Gwenae Le Moal, D. Neau, L. Alleman, C. Cazanave, E. Lazaro, P. Duffau, A. Riché, Y Gérard, G. Barrière, Sandrine Reigadas, M.‐A. Vandenhende, F. Bonnet   +15 more
openalex   +2 more sources

Arylamide Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1997
Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency.
He Zhao, Nouri Neamati, Abhijit Mazumder, Sanjay Sunder, Yves Pommier, Terrence R. Burke   +5 more
openalex   +3 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

Weight change with antiretroviral switch from integrase inhibitor or tenofovir alafenamide-based to Doravirine-Based regimens in people with HIV [PDF]

HIV Research & Clinical Practice
Background Weight gain has been well-described with integrase strand transfer inhibitors (INSTIs) and tenofovir alafenamide (TAF). Doravirine (DOR) has been identified as a relatively “weight-neutral” drug; however, there is little data describing its ...
Arianna E. Kousari, Melissa P. Wilson, Kellie L. Hawkins, Mohamed Mehdi Bandali, Andrés F. Henao-Martínez, Edward M. Gardner, Kristine M. Erlandson   +6 more
doaj   +2 more sources

Weight gain and integrase inhibitors [PDF]

Current Opinion in Infectious Diseases, 2020
Purpose of review Weight gain and obesity among people living with HIV (PLWH) is a serious problem that occurs often after initiation of antiretroviral therapy but may be worse with integrase strand transfer inhibitors (INSTIs).
Allison Ross, Eckard, Grace A, McComsey
openaire   +2 more sources

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.
Mathieu Métifiot, Christophe Marchand, Kasthuraiah Maddali, Yves Pommier   +3 more
openaire   +3 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