Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
Viruses, 2010 The HIV-1 integrase enzyme is essential for integrating the viral DNA into the host chromosome. Infection is aborted in the absence of integration, making integrase an attractive antiviral target. Recently approved inhibitors of integrase bind tightly to
Robert Craigie, Zhiqi Yin
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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
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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
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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
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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
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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
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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
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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
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How developing world concerns need to be part of drug development plans: A case study of four emerging antiretrovirals [PDF]
, 2008 Clinical trials are usually designed to meet registration requirements in developed countries, and do not always address key concerns for use in developing countries.
Alexandra Calmy +22 more
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Synthesis of an Atropisomeric HIV Integrase Inhibitor [PDF]
Synfacts, 2015 Philip Kocieński
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