Multifaceted HIV integrase functionalities and therapeutic strategies for their inhibition
AN Engelman - Journal of Biological Chemistry, 2019 - ASBMB
Antiretroviral inhibitors that are used to manage HIV infection/AIDS predominantly target
three enzymes required for virus replication: reverse transcriptase, protease, and integrase …
three enzymes required for virus replication: reverse transcriptase, protease, and integrase …
Multimodal functionalities of HIV-1 integrase
AN Engelman, M Kvaratskhelia - Viruses, 2022 - mdpi.com
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 …
genomes. Co-packaged with viral RNA and reverse transcriptase into capsid-encased viral …
[HTML][HTML] HIV-1 integrase binds the viral RNA genome and is essential during virion morphogenesis
JJ Kessl, SB Kutluay, D Townsend, S Rebensburg… - Cell, 2016 - cell.com
While an essential role of HIV-1 integrase (IN) for integration of viral cDNA into human
chromosome is established, studies with IN mutants and allosteric IN inhibitors (ALLINIs) …
chromosome is established, studies with IN mutants and allosteric IN inhibitors (ALLINIs) …
Discovery of BI 224436, a noncatalytic site integrase inhibitor (NCINI) of HIV-1
LD Fader, E Malenfant, M Parisien… - ACS medicinal …, 2014 - ACS Publications
An assay recapitulating the 3′ processing activity of HIV-1 integrase (IN) was used to
screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization …
screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization …
A new class of multimerization selective inhibitors of HIV-1 integrase
The quinoline-based allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are promising
candidates for clinically useful antiviral agents. Studies using these compounds have …
candidates for clinically useful antiviral agents. Studies using these compounds have …
Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells
M Balakrishnan, SR Yant, L Tsai, C O'Sullivan… - PloS one, 2013 - journals.plos.org
HIV-1 integrase (IN) is the target for two classes of antiretrovirals: i) the integrase strand-
transfer inhibitors (INSTIs) and ii) the non-catalytic site integrase inhibitors (NCINIs). NCINIs …
transfer inhibitors (INSTIs) and ii) the non-catalytic site integrase inhibitors (NCINIs). NCINIs …
Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage
E Le Rouzic, D Bonnard, S Chasset, JM Bruneau… - Retrovirology, 2013 - Springer
Abstract Background LEDGF/p75 (LEDGF) is the main cellular cofactor of HIV-1 integrase
(IN). It acts as a tethering factor for IN, and targets the integration of HIV in actively …
(IN). It acts as a tethering factor for IN, and targets the integration of HIV in actively …
Distribution and redistribution of HIV-1 nucleocapsid protein in immature, mature, and integrase-inhibited virions: a role for integrase in maturation
During virion maturation, HIV-1 capsid protein assembles into a conical core containing the
viral ribonucleoprotein (vRNP) complex, thought to be composed mainly of the viral RNA …
viral ribonucleoprotein (vRNP) complex, thought to be composed mainly of the viral RNA …
Structural basis for inhibitor-induced aggregation of HIV integrase
K Gupta, V Turkki, S Sherrill-Mix, Y Hwang, G Eilers… - PLoS …, 2016 - journals.plos.org
The allosteric inhibitors of integrase (termed ALLINIs) interfere with HIV replication by
binding to the viral-encoded integrase (IN) protein. Surprisingly, ALLINIs interfere not with …
binding to the viral-encoded integrase (IN) protein. Surprisingly, ALLINIs interfere not with …
Integrase-RNA interactions underscore the critical role of integrase in HIV-1 virion morphogenesis
JL Elliott, JE Eschbach, PC Koneru, W Li… - Elife, 2020 - elifesciences.org
A large number of human immunodeficiency virus 1 (HIV-1) integrase (IN) alterations,
referred to as class II substitutions, exhibit pleiotropic effects during virus replication …
referred to as class II substitutions, exhibit pleiotropic effects during virus replication …