1E7-03, a low MW compound targeting host protein phosphatase-1, inhibits HIV-1 transcription

Authors

Tatyana Ammosova, The Center For Sickle Cell Disease
Maxim Platonov, Taras Shevchenko National University of Kyiv
Andrei Ivanov, The Center For Sickle Cell Disease
Yasemin Saygideʇer Kont, Georgetown Lombardi Comprehensive Cancer Center
Namita Kumari, The Center For Sickle Cell Disease
Kylene Kehn-Hall, George Mason University - Science and Technology Campus
Marina Jerebtsova, Childrens National Health System
Amol A. Kulkarni, Howard University
Aykut Üren, Georgetown Lombardi Comprehensive Cancer Center
Dmytro Kovalskyy, Taras Shevchenko National University of Kyiv
Sergei Nekhai, The Center For Sickle Cell Disease

Document Type

Article

Publication Date

1-1-2014

Abstract

Background and purpose: HIV-1 transcription is activated by the Tat protein which recruits the cyclin-dependent kinase CDK9/cyclin T1 to TAR RNA. Tat binds to protein phosphatase-1 (PP1) through the Q35VCF38 sequence and translocates PP1 to the nucleus. PP1 dephosphorylates CDK9 and activates HIV-1 transcription. We have synthesized a low MW compound 1H4, that targets PP1 and prevents HIV-1 Tat interaction with PP1 and inhibits HIV-1 gene transcription. Here, we report our further work with the 1H4-derived compounds and analysis of their mechanism of action.

Recommended Citation

Ammosova, Tatyana; Platonov, Maxim; Ivanov, Andrei; Kont, Yasemin Saygideʇer; Kumari, Namita; Kehn-Hall, Kylene; Jerebtsova, Marina; Kulkarni, Amol A.; Üren, Aykut; Kovalskyy, Dmytro; and Nekhai, Sergei, "1E7-03, a low MW compound targeting host protein phosphatase-1, inhibits HIV-1 transcription" (2014). The Center For Sickle Cell Disease Faculty Publications. 64.
https://dh.howard.edu/sicklecell_fac/64