HIV Integrase Inhibitors Block Replication of Alpha-, Beta-, and Gammaherpesviruses [PDF]
mBio, 2014 The catalytic site of the HIV integrase is contained within an RNase H-like fold, and numerous drugs have been developed that bind to this site and inhibit its activity.
Zhipeng Yan +8 more
doaj +6 more sources
Pharmacology of HIV integrase inhibitors. [PDF]
Curr Opin HIV AIDS, 2012 The purpose of this paper is to review recent and relevant pharmacology data for three HIV integrase inhibitors: raltegravir (marketed), dolutegravir and elvitegravir (both in Phase III drug development).
Adams JL, Greener BN, Kashuba AD.
europepmc +7 more sources
Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes [PDF]
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 +7 more
doaj +5 more sources
Investigation of furo[2,3-h]- and pyridazino[3,4-f]cinnolin-3-ol scaffolds as substrates for the development of novel HIV-1 integrase inhibitors [PDF]
, 2011 With the aim to develop novel HIV-1 integrase inhibitors, we obtained a set of condensed ring systems based on the furo[2,3-h]cinnolin-3(2H)-one and pyridazino[3,4-f]cinnolin-3-ol scaffolds bearing a potential chelating pharmacophore, which can be ...
Casule, Paola +7 more
core +3 more sources
HIV/HCV-coinfection: which role can new antiretrovirals such as integrase inhibitors play? [PDF]
European Journal of Medical Research, 2009 End-stage liver disease has become one of the most frequent causes of death in HIV/HCV-coinfected patients. The role of new antiretrovirals in the progression of liver fibrosis has yet to be defined.
Vogel Martin, Nelson Mark
doaj +2 more sources
Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: A single mode of inhibition for the three HIV enzymes? [PDF]
, 2006 The genome of human immunodeficiency virus type 1 (HIV-1) encodes 15 distinct proteins, three of which provide essential enzymatic functions: a reverse transcriptase (RT), an integrase (IN), and a protease (PR).
Camarasa Rius, María José +4 more
core +4 more sources
Biomath, 2012 Antiviral combination therapies consisting of reverse transcriptase inhibitors, protease inhibitors and an integrase inhibitor, have been developed to suppress HIV below the limit of detection.
Dimitra Bon +3 more
doaj +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 +4 more
doaj +1 more source
Molecules, 2023 As an important antiviral target, HIV-1 integrase plays a key role in the viral life cycle, and five integrase strand transfer inhibitors (INSTIs) have been approved for the treatment of HIV-1 infections so far.
Yu-Chan Wang +8 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 +18 more
doaj +1 more source