PCAF公司
乙酰化
组蛋白
乙酰转移酶
细胞生物学
溴尿嘧啶
化学
小分子
转录因子
P300-CBP转录因子
组蛋白乙酰转移酶
辅活化剂
乙酰转移酶
生物
组蛋白乙酰转移酶
BRD4
分子生物学
CREB结合蛋白
癌症研究
信号转导
生物化学
基因
奶油
作者
Rahul Modak,Jeelan Basha,Narendra Bharathy,Koustav Maity,Pushpak Mizar,Akshay Bhat,Madavan Vasudevan,Vinay Kumar Rao,Wai Kay Kok,Nagashayana Natesh,Reshma Taneja,Tapas K. Kundu
摘要
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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