Bromodomain(BRD)
A bromodomain is an approximately 110 amino acid protein domain that recognizes acetylated lysine residues, such as those on the N-terminal tails of histones. Bromodomains are responsible in transducing the signal carried by acetylated lysine residues and translating it into various normal or abnormal phenotypes. Bromodomain-containing proteins can have a wide variety of functions, ranging from histone acetyltransferase activity and chromatin remodeling to transcriptional mediation and co-activation.
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I-BET-762是一种BET (bromodomain and extra terminal domain)蛋白抑制剂， IC50约为35 nM，抑制巨噬细胞产生促炎蛋白，抑制急性炎症，对其他溴区结合域包含的蛋白具有高度的选择性。
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PFI-1 (PF-6405761)是一种选择性的BET(溴区包含蛋白)抑制剂，抑制BRD4时IC50为0.22 μM。
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RVX-208是一种有效的BET bromodomain抑制剂，作用于BD2， IC50为0.510 μM，比作用于BD1选择性高170倍。
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SGC-CBP30是CREBBP和EP300的布罗莫结构域抑制剂，IC50分别为21-69nM和38 nM。
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I-BET151(GSK1210151A)是BET布罗莫结构域抑制剂，对BRD4的pIC50为6.1。
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