Novel therapeutic strategies targeting HIV integrase [PDF]
BMC Medicine, 2012 Abstract Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an obvious and attractive therapeutic strategy.
Richard D Sloan +2 more
openaire +5 more sources
Assessing weight change in adolescents and young adults with perinatally acquired HIV and integrase inhibitor use. [PDF]
HIV MedAbstract Introduction Integrase strand transfer inhibitors (INSTIs) are the mainstay of treatment in adults and children living with HIV. Weight gain has been associated with INSTI use in adults; however, less data exist on its effects on younger patients.
Pincus KJ +6 more
europepmc +2 more sources
Alternaria alternata (Fr) Keissl Crude Extract Inhibits HIV Subtypes and Integrase Drug-Resistant Strains at Different Stages of HIV Replication [PDF]
PharmaceuticalsBackground/Objectives: The development of HIV drug resistance to current antiretrovirals, and the antiretrovirals’ inability to cure HIV, provides the need of developing novel drugs that inhibit HIV-1 subtypes and drug-resistance strains.
Darian Naidu +4 more
doaj +2 more sources
Exploring Zinc C295 as a Dual HIV-1 Integrase Inhibitor: From Strand Transfer to 3′-Processing Suppression [PDF]
PharmaceuticalsBackground: The global AIDS pandemic highlights the urgent need for novel antiretroviral therapies (ART). In our previous work, Zinc C295 was identified as a potent HIV-1 integrase strand transfer (ST) inhibitor. This study explores its potential to also
Sharif Karim Sayyed +8 more
doaj +2 more sources
Treatment of HIV Infections with HIV Integrase Inhibitors [PDF]
ACS Medicinal Chemistry Letters, 2016 Abdel-Magid AF.
openaire +4 more sources
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
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
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
Integrase deficient lentiviral vector: prospects for safe clinical applications [PDF]
PeerJ, 2022 HIV-1 derived lentiviral vector is an efficient transporter for delivering desired genetic materials into the targeted cells among many viral vectors. Genetic material transduced by lentiviral vector is integrated into the cell genome to introduce new ...
Chee-Hong Takahiro Yew +6 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