Multimodal Functionalities of HIV-1 Integrase [PDF]
Viruses, 2022 Integrase is the retroviral protein responsible for integrating reverse transcripts into cellular genomes. Co-packaged with viral RNA and reverse transcriptase into capsid-encased viral cores, human immunodeficiency virus 1 (HIV-1) integrase has long ...
Alan N. Engelman, Mamuka Kvaratskhelia
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HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure [PDF]
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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The Discovery of Indole-2-carboxylic Acid Derivatives as Novel HIV-1 Integrase Strand Transfer Inhibitors [PDF]
Molecules, 2023 As an important antiviral target, HIV-1 integrase plays a key role in the viral life cycle, and five integrase strand transfer inhibitors (INSTIs) have been approved for the treatment of HIV-1 infections so far.
Yu-Chan Wang +8 more
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CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones [PDF]
E-Journal of Chemistry, 2010 To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
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The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function [PDF]
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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Evaluation of a flavonoid library for inhibition of interaction of HIV-1 integrase with human LEDGF/p75 towards a structure–activity relationship [PDF]
Annals of Medicine, 2022 Background: Proteinśprotein interaction (PPI) between lens epithelium-derived growth factor (LEDGF/p75) and human immunodeficiency virus (HIV) integrase (IN) becomes an attractive target for anti-HIV drug development.Methods: The blockade of this ...
Zhi-Hui Yin +4 more
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Exploring Zinc C295 as a Dual HIV-1 Integrase Inhibitor: From Strand Transfer to 3′-Processing Suppression [PDF]
PharmaceuticalsBackground: The global AIDS pandemic highlights the urgent need for novel antiretroviral therapies (ART). In our previous work, Zinc C295 was identified as a potent HIV-1 integrase strand transfer (ST) inhibitor. This study explores its potential to also
Sharif Karim Sayyed +8 more
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Structural Impact of Ex Vivo Resistance Mutations on HIV-1 Integrase Polymers Induced by Allosteric Inhibitors. [PDF]
J Mol BiolMontermoso S +7 more
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The HIV-1 Integrase C-Terminal Domain Induces TAR RNA Structural Changes Promoting Tat Binding. [PDF]
Int J Mol Sci, 2022 Rocchi C +10 more
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HIV-2 integrase variation in integrase inhibitor-naïve adults in Senegal, West Africa. [PDF]
PLoS ONE, 2011 Antiretroviral therapy for HIV-2 infection is hampered by intrinsic resistance to many of the drugs used to treat HIV-1. Limited studies suggest that the integrase inhibitors (INIs) raltegravir and elvitegravir have potent activity against HIV-2 in ...
Geoffrey S Gottlieb +18 more
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