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 +5 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 +5 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 +5 more
openalex +3 more sources
Retrovirus-based pseudotyped virus neutralisation assays overestimate neutralising activity in sera from participants receiving integrase inhibitors [PDF]
Scientific ReportsRetroviral pseudotype-based virus neutralisation assays are widely used to estimate functional immunity, but may be unsuitable for testing human immunodeficiency virus (HIV)-infected individuals receiving integrase inhibitor treatment. We evaluated these
Mhairi J. McCormack +11 more
doaj +2 more sources
Allosteric HIV Integrase Inhibitors Promote Formation of Inactive Branched Polymers via Homomeric Carboxy-Terminal Domain Interactions. [PDF]
Structure, 2021 Gupta K +10 more
europepmc +3 more sources
Treatment of HIV Infections with HIV Integrase Inhibitors. [PDF]
ACS Med Chem Lett, 2017 Abdel-Magid AF.
europepmc +4 more sources
Raltegravir: first in class HIV integrase inhibitor
Therapeutics and Clinical Risk Management, 2008 Zelalem Temesgen1, Dawd S Siraj21Mayo Clinic, Rochester, MN, USA; 2East Carolina University Greenville, NC, USAAbstract: On October 16, 2007, the US Food and Drug Administration (FDA) approved raltegravir for treatment of human immunodeficiency virus ...
Zelalem Temesgen, Dawd S Siraj
doaj +4 more sources
Feasibility of Switching to an Integrase Inhibitor-Based Single-Tablet Regimen in Adults Living With HIV and Sustained Virological Suppression on Outdated Antiretroviral Therapies. [PDF]
CureusTiecco G +7 more
europepmc +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