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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OTX-015是新型BRD2/3/4抑制剂，对一些B细胞肿瘤细胞株有抗增殖活性，对DLBCL 细胞的IC50为192nM。
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(+)-JQ1, an active enantiomer of JQ1, is a potent, highly specific and Kac-competitive inhibitor of bromodomain and extraterminal domain (BET) proteins, blocks BRD4 resulting in inhibition of c-Myc expression and tumor growth. (+)-JQ1是一种BET bromodomain抑制剂，作用于BRD4(2)，IC50为33 nM，结合到BET家族的所有Bromodomain结构域，而不结合到BET家族以外的Bromodomain结构域。
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GSK1324726A (I-BET726)是新型的BET蛋白抑制剂，对BRD2，BRD3和BRD4的IC50分别为41 nM，31 nM和22 nM。
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OF-1是BRPF1B和BRPF2 bromodomain抑制剂，Kd值分别为100nM和500nM，对BRD4结合能力弱39倍。
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Bromosporine是一种广谱bromodomains抑制剂，作用于BRD2， BRD4， BRD9和CECR2，IC50分别为0.41 μM， 0.29 μM， 0.122 μM和0.017 μM 。
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