期刊
ACS CHEMICAL BIOLOGY
卷 8, 期 6, 页码 1311-1323出版社
AMER CHEMICAL SOC
DOI: 10.1021/cb4000597
关键词
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资金
- Department of Biotechnology, Govt. of India [BT/01/CEIB/10/111/01]
- National Agricultural Innovative Project (NAIP), Indian Council of Agricultural Research, New Delhi, Govt. of India [NAIP/Comp-4/C-30017/2008-09]
- JNCASR
- Sir J. C. Bose National Fellowship
- Department of Science & Technology, Govt. of India
- National Medical Research Council
- A*STAR Singapore Stem Cell Consortium
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.
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