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Integrase

Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach

41 views | Sep 08 2021

Zahra Molavi et al. recommended further experimental evaluations in vitro and in vivo on FDA-approved drugs to assess their potential antiviral effect on SARS-CoV-2. [Read the Full Post]

Molecular dynamic simulations to investigate the structural impact of known drug resistance mutations on HIV-1C Integrase-Dolutegravir binding

97 views | Aug 24 2020

Rumbidzai Chitongo et al. suggested the G140S mutant had the strongest effect on the HIV-1C IN protein structure and Dolutegravir binding. [Read the Full Post]

Safety and efficacy of elvitegravir, dolutegravir, and raltegravir in a real-world cohort of treatment-naïve and -experienced patients

436 views | Nov 06 2019

Brehm TT et al. showed that side effects were only rarely observed and generally mild in all subgroups. In light of a slightly higher incidence of vertigo and sleep disturbances in patients switched to DTG, awareness of the potential onset of psychiatric symptoms is warranted during follow-up in those patients. [Read the Full Post]

Raltegravir (MK-0518): an integrase inhibitor for the treatment of HIV-1

281 views | Jun 20 2019

Evering TH et al. indicated it has demonstrated a favorable side-effect profile in treatment-naive and -experienced patients and a subset of heavy treatment-experienced patients have been able a achieve virologic suppression with raltegravir as part of combination therapy despite limited treatment options. [Read the Full Post]

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor

307 views | May 28 2019

Kobayashi M et al. demonstrated that S/GSK1349572 would be classified as a next-generation drug in the integrase inhibitor class, with a resistance profile markedly different from that of first-generation integrase inhibitors. [Read the Full Post]

Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial

368 views | May 08 2019

Sax PE et al. indicated at 48 weeks, virological suppression with the bictegravir regimen was achieved and was non-inferior to the dolutegravir regimen in previously untreated adults. There was no emergent resistance to either regimen. The fixed-dose combination of bictegravir, emtricitabine, and tenofovir alafenamide was safe and well tolerated compared with the dolutegravir regimen. [Read the Full Post]

Susceptibility of porcine endogenous retrovirus to anti-retroviral inhibitors

574 views | Apr 09 2018

Argaw T et al. indicated that some of the licensed anti-retroviral drugs may be useful for controlling PERV infection. However, the efficacy at nanomolar concentrations put forward integrase inhibitors as a drug that has the potential to be useful in the event that xenotransplantation recipients have evidence of PERV transmission and replication. [Read the Full Post]

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H

786 views | Jan 11 2018

Corona A et al. provided new structural information to modulate IN and RNase H inhibitory activities for development of dual-acting anti-HIV agents. [Read the Full Post]

Cryo-EM reveals a novel octameric integrase structure for betaretroviral intasome function

1126 views | Jun 17 2017

Ballandras-Colas A et al. revealed a novel octameric integrase structure for betaretroviral intasome function. [Read the Full Post]

Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site

1110 views | May 13 2017

Métifiot M et al. indicated that the conserved residue Q146 in the flexible loop of HIV-1 integrase is critical for productive viral DNA binding through specific contacts with the virus DNA ends in the 3'-processing and ST reactions. [Read the Full Post]