mBio, 2017 Resistance to the integrase strand transfer inhibitors raltegravir and elvitegravir is often due to well-identified mutations in the integrase gene. However, the situation is less clear for patients who fail dolutegravir treatment.
Isabelle Malet +7 more
doaj +1 more source
The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function
mBio, 2023 Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer +14 more
doaj +1 more source
Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids
Molecules, 2015 HIV integrase, encoded at the 3′-end of the HIV pol gene, is essential for HIV replication. This enzyme catalyzes the incorporation of HIV DNA into human DNA, which represents the point of “no-return” in HIV infection.
Vasu Nair, Maurice Okello
doaj +1 more source
Resistance to novel drug classes [PDF]
, 2009 Understanding the mechanisms that underlie resistance development to novel drugs is essential to a better clinical management of resistant viruses and to prevent further resistance development and spread. RECENT FINDINGS: Integrase inhibitors and CCR5
Calvez, V. +3 more
core +1 more source
Nonhuman Primates and Humanized Mice for Studies of HIV-1 Integrase Inhibitors: A Review
Pathogens and Immunity, 2016 Since the discovery of the first inhibitors of HIV replication, drug resistance has been a major problem in HIV therapy, due, in part, to the high mutation rate of HIV.
Said A. Hassounah +2 more
doaj +1 more source
Anti-HIV therapy: pipeline approaches and future directions [PDF]
, 2011 Human immunodeficiency virus (HIV), with about 30 million deaths and double infections (in developing countries), is an open challenge today for global scientists.
Lavkush Dwivedi, Mansi Shrivastava
core +2 more sources
HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure
Retrovirology, 2009 In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin +5 more
doaj +1 more source
The Evolution of Drug Resistance Interpretation Algorithms: ANRS, REGA and Extension of Resistance Analysis to HIV-1 Group O and HIV-2 [PDF]
, 2012 Antiretroviral drug resistance is mostly linked to a complex interaction of several amino acids with variable importance or a single amino acid. To facilitate the interpretation of observed mutation patterns, hospital university centers have developed ...
Eberle, Josef, Gürtler, Lutz
core +1 more source
Switching from a protease inhibitor-based regimen to a dolutegravir-based regimen : a randomized clinical trial to determine the effect on peripheral blood and ileum biopsies from antiretroviral therapy-suppressed human immunodeficiency virus-infected individuals [PDF]
, 2018 Background: Optimization of combination antiretroviral therapy (cART) can impact the human immunodeficiency virus (HIV) reservoir. We evaluated the effect on the HIV reservoir in peripheral blood and ileum biopsies in patients switching from boosted ...
Blanco, Julià +15 more
core +3 more sources
Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity
South African Journal of Science, 2018 Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams +4 more
doaj +1 more source