Results 31 to 40 of about 17,322 (222)
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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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
doaj +1 more source
Molecular features related to HIV integrase inhibition obtained from structure- and ligand-based approaches. [PDF]
PLoS ONE, 2014 Among several biological targets to treat AIDS, HIV integrase is a promising enzyme that can be employed to develop new anti-HIV agents. The aim of this work is to propose a mechanistic interpretation of HIV-1 integrase inhibition and to rationalize the ...
Luciana L de Carvalho +5 more
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HIV Dynamics and Integrase Inhibitors
Antiviral Chemistry and Chemotherapy, 2009 The integrase inhibitor (INI) raltegravir has shown promising results in clinical trials to date, reducing second phase HIV RNA levels by 70% in comparison with standard regimens. These trial results have been limited by the 50 copies/ml detection limit of the HIV RNA assay and have not investigated the effect of an INI regimen on levels of latently ...
openaire +2 more sources
Protease mediated maturation of HIV: Inhibitors of protease and the maturation process [PDF]
, 2012 Protease-mediated maturation of HIV-1 virus particles is essential for virus infectivity. Maturation occurs concomitant with immature virus particle release and is mediated by the viral protease (PR), which sequentially cleaves the Gag and Gag-Pol ...
Catherine S. Adamson +1 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
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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, 2013 This chapter presents the discovery, development and evolution of integrase strand transfer inhibitors. A brief overview of the first‐generation inhibitors raltegravir and elvitegravir serves to describe their landmark advancement of the field and also outline areas for further improvement.
Brian A. Johns +2 more
openaire +4 more sources
Resistance to inhibitors of the human immunodeficiency virus type 1 integration
Brazilian Journal of Infectious DiseasesThis review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 ...
Daria J Hazuda
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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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