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Probing p300/CBP associated Factor (PCAF)-dependent pathways with a small molecule inhibitor

Modak, Rahul and Basha, Jeelan and Bharathy, Narendra and Maity, Koustav and Mizar, Pushpak and Bhat, Akshay V and Vasudevan, Madavan and Rao, Vinay Kumar and Kok, Wai Kay and Natesh, Nagashayana and Taneja, Reshma and Kundu, Tapas K (2013) Probing p300/CBP associated Factor (PCAF)-dependent pathways with a small molecule inhibitor. In: ACS Chemical Biology, 8 (6). pp. 1311-1323.

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Official URL: http://dx.doi.org/10.1021/cb4000597

Abstract

PCAF (KAT2B) belongs to the GNAT family of lysine acetyltransferases (KAT) and specifically acetylates the histone H3K9 residue and several nonhistone proteins. PCAF is also a transcriptional coactivator. Due to the lack of a PCAF KAT-specific small molecule inhibitor, the exclusive role of the acetyltransferase activity of PCAF is not well understood. Here, we report that a natural compound of the hydroxybenzoquinone class, embelin, specifically inhibits H3Lys9 acetylation in mice and inhibits recombinant PCAF-mediated acetylation with near complete specificity in vitro. Furthermore, using embelin, we have identified the gene networks that are regulated by PCAF during muscle differentiation, further highlighting the broader regulatory functions of PCAF in muscle differentiation in addition to the regulation via MyoD acetylation.

Item Type: Journal Article
Additional Information: Copyright of this article belongs to American Chemical Society.
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Depositing User: Francis Jayakanth
Date Deposited: 20 Sep 2013 12:12
Last Modified: 20 Sep 2013 12:12
URI: http://eprints.iisc.ac.in/id/eprint/47223

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