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Reactivation of latent HIV-1 provirus via targeting protein phosphatase-1.


ABSTRACT:

Background

HIV-1 escapes antiretroviral drugs by integrating into the host DNA and forming a latent transcriptionally silent HIV-1 provirus. This provirus presents the major hurdle in HIV-1 eradication and cure. Transcriptional activation, which is prerequisite for reactivation and the eradication of latent proviruses, is impaired in latently infected T cells due to the lack of host transcription factors, primarily NF-κB and P-TEFb (CDK9/cyclin T1). We and others previously showed that protein phosphatase-1 (PP1) regulates HIV-1 transcription by modulating CDK9 phosphorylation. Recently we have developed a panel of small molecular compounds targeting a non-catalytic site of PP1.

Results

Here we generated a new class of sulfonamide-containing compounds that activated HIV-1 in

SUBMITTER: Tyagi M 

PROVIDER: S-EPMC4504130 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature