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Effect of transcription peptide inhibitors on HIV-1 replication
Journal article   Open access   Peer reviewed

Effect of transcription peptide inhibitors on HIV-1 replication

Rachel Van Duyne, Jessica Cardenas, Rebecca Easley, Weilin Wu, Kylene Kehn-Hall, Zak Klase, Susana Mendez, Chen Zeng, Hao Chen, Mohammed Saifuddin, …
Virology (New York, N.Y.), v 376(2), pp 308-322
05 Jul 2008
PMID: 18455747
url
https://doi.org/10.1016/j.virol.2008.02.036View
Published, Version of Record (VoR) Restricted

Abstract

Cell cycle Computer modeling Cyclin-dependent kinase HIV PBMC Peptide inhibitor Small animal model Stem cells Tat Transcription
HIV-1 manipulates cellular machineries such as cyclin dependent kinases (cdks) and their cyclin elements, to stimulate virus production and maintain latent infection. Specifically, the HIV-1 viral protein Tat increases viral transcription by binding to the TAR promoter element. This binding event is mediated by the phosphorylation of Pol II by complexes such as cdk9/Cyclin T and cdk2/Cyclin E. Recent studies have shown that a Tat 41/44 peptide derivative prevents the loading of cdk2 onto the HIV-1 promoter, inhibiting gene expression and replication. Here we show that Tat peptide analogs computationally designed to dock at the cyclin binding site of cdk2 have the ability to bind to cdk2 and inhibit the association of cdk2 with the HIV promoter. Specifically, the peptide LAALS dissociated the complex and decreased kinase activity in vitro. We also describe our novel small animal model which utilizes humanized Rag2 −/−γ c −/− mice. This small peptide inhibitor induces a decrease in HIV-1 viral transcription in vitro and minimizes viral loads in vivo.

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Collaboration types
Domestic collaboration
Web of Science research areas
Virology
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