Virology Mechanism of action of allosteric HIV-1 integrase inhibitors THE OHIO STATE UNIVERSITY Mamuka Kvaratskhelia SlaughterAlison PaigeAn essential step in the HIV-1 replication cycle is the integration of the viral DNA into the host chromatin, which is catalyzed by the viral enzyme integrase (...
Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors J. Biol. Chem. (2012) March, 21, 10.1074/jbc.M112.354373 Google Scholar Cited by (145) Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved re...
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are a very promising new class of anti-HIV-1 agents that exhibit a multimodal mechanism of action by allosterically modulating IN multimerization and interfering with IN-lens epithelium-derived growth factor (LEDGF)/p75 binding. Selection of vi...
HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand... Investigates the mechanism of action of diketo acid (DKA), a novel class of HIV-1 antiviral agent that selectively block the strand transfer activity of in... Espeseth,Amy,S.,... - 《Proceedings...
3. Dolutegravir: A next-generation integrase inhibitor for treatment of HIV infection [J] . OsterholzerD.A., GoldmanM. Clinical infectious diseases . 2014,第2期 机译:Dolutegravir:用于治疗HIV感染的新一代整合酶抑制剂 4. Characterization of the mechanism of action of allosteric inhibitors for...
The integrase strand transfer inhibitors (INSTIs) are the newest antiretroviral class in the HIV treatment armamentarium. Dolutegravir (DTG) is the only se
However, the current three clinical IN inhibitors, raltegravir, elvitegravir and dolutegravir share the same inhibitory mechanism, resulting in a common clinical resistance profile which have emerged in infected patients receiving treatment. Therefore, it is important to develop small molecule inhibitors ...
Presented is a review of computer-aided drug design efforts targeting HIV IN. Included is an overview of the lifecycle of HIV, with emphasis on the mechanism of action of IN, biological assays for measuring IN activity and identifying IN inhibitors, and the appropriate cell-based assays required...
Multimodal mechanism of action of allosteric HIV-1 integrase inhibitors. Integrase (IN) is required for lentivirus replication and is a proven drug target for the prevention of AIDS in HIV-1-infected patients. While clinical str... Kellie,Ann,Jurado,... - 《Expert Reviews in Molecular Medicine...
These data suggest that the allosteric inhibitors of IN are promising antiviral agents and provide new information on their mechanism of action.Previous article in issue Next article in issue Bioinformatics Biophysics Genomics Retrovirus X-ray Crystallography Analytical Ultracentrifugation (AUC) Oligomerization...