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.
Mathieu Métifiot +3 more
doaj +5 more sources
Two cases of possible transmitted HIV drug resistance to all currently available integrase inhibitors, the Netherlands, 2025 [PDF]
EurosurveillanceTransmitted integrase inhibitor resistance in newly diagnosed HIV remains rare. We report two cases with baseline resistance to all currently available integrase inhibitors in the Netherlands in 2025.
Marc van der Valk
doaj +2 more sources
Weight gain and integrase inhibitors. [PDF]
Curr Opin Infect Dis, 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).
Eckard AR, McComsey GA.
europepmc +4 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
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
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
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
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 +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 +15 more
doaj +1 more source