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 +3 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
Authentic HIV-1 Integrase Inhibitors [PDF]
Future Medicinal Chemistry, 2010 HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Chenzhong, Liao +4 more
openaire +2 more sources
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