溴结构域(bromodomain，BD)是一种高度保守的蛋白质结构域，具有特异性识别结合乙酰化赖氨酸残基的生物学功能。溴结构域蛋白4(bromodomain-containing protein 4，BRD4)是溴结构域和超末端结构(bromodomain and extra-terminal domain，BET)家族成员之一，因对基因转录具有强大的调控能力而受到较多关注。目前，靶向BRD4的小分子抑制剂在抗炎和抗癌领域展现出巨大的潜力。本文介绍了 BRD4的生物学功能和在人体组织中的表达分布，结合BRD4抑制剂的药物研发现状重点阐述BRD4抑制剂在炎症性疾病中的作用。
Research advances of BRD4 and its inhibitors in inflammatory diseases
The bromodomain(BD)is a highly conserved protein structural domain that has the biological function of specifically recognizing and binding acetylated lysine residues.The bromodomain-containing protein 4(BRD4)is a member of the bromodomain and extra-terminal domain(BET)family,which has received much attention for its powerful ability to regulate gene transcription.Currently,small molecule inhibitors targeting BRD4 have shown great potential in anti-inflamma-tory and anti-cancer fields.This paper described the biological function and distribution of BRD4 in human tissues,summa-rizes the current status of drug development of BRD4 inhibitors,and focuses on the role of BRD4 inhibitors in inflammatory diseases.
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