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Title: Specific Inhibition of p300-HAT Alters Global Gene Expression and Represses HIV Replication
Authors: Mantelingu, K
Reddy, B A Ashok
Swaminathan, V
Hari Kishore, A
Siddappa, Nagadenahalli B
Pavan Kumar, G V
Nagashankar, G
Natesh, Nagashayana
Roy, Siddhartha
Sadhale, Parag P
Ranga, Udaykumar
Narayana, Chandrabhas
Kundu, Tapas K
Keywords: Histone Acetyltransferase Activity
Transcriptional Regulation
Issue Date: Jun-2007
Publisher: Cell Press
Citation: Chemistry & Biology 14(6), 645-657 (2007)
Abstract: Reversible acetylation of histone and nonhistone proteins plays pivotal role in cellular homeostasis. Dysfunction of histone acetyltransferases (HATs) leads to several diseases including cancer, neurodegenaration, asthma, diabetes, AIDS, and cardiac hypertrophy. We describe the synthesis and characterization of a set of p300-HAT-specific small-molecule inhibitors from a natural nonspecific HAT inhibitor, garcinol, which is highly toxic to cells. We show that the specific inhibitor selectively represses the p300-mediated acetylation of p53 in vivo. Furthermore, inhibition of p300-HAT down regulates several genes but significantly a few important genes are also upregulated. Remarkably, these inhibitors were found to be nontoxic to T cells, inhibit histone acetylation of HIV infected cells, and consequently inhibit the multiplication of HIV.
Description: Restricted Access
Other Identifiers: 1074-5521
Appears in Collections:Research Papers (Tapas K. Kundu)

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