Role of the HIV-1 Positive Elongation Factor P-TEFb and Inhibitors Thereof

Author(s): Yan Wang, Xin-yong Liu, Erik De Clercq.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 9 , Issue 3 , 2009

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Abstract:

Transcription is considered to be a crucial step in the replication cycle of HIV-1. Tat regulates an early step of transcription elongation. The positive elongation factor P-TEFb, a heterodimer containing a catalytic subunit (CDK9) and unique regulatory cyclins (CycT1), is required for HIV-1 Tat transcriptional activation. This is a potential target for new HIV-1 transcription inhibitors. Without P-TEFb, transactivation is restrained and only short transcripts are generated. All the P-TEFb inhibitors can suppress the HIV-1 transactivation process by inhibition of CycT1, CDK9 or their interaction. Several low-molecular-weight compounds such as flavopiridol, roscovitine and the human small nuclear RNA 7SK which have been showed to possess potent anti-HIV activity by interfering with P-TEFb functions are reviewed in this article.

Keywords: HIV-1, Tat, TAR, P-TEFb, transcription inhibitor

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Article Details

VOLUME: 9
ISSUE: 3
Year: 2009
Page: [379 - 385]
Pages: 7
DOI: 10.2174/1389557510909030379
Price: $58

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