溴结构域蛋白4及其抑制剂在炎症性疾病中的研究进展

Research advances of BRD4 and its inhibitors in inflammatory diseases

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。

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-inflammatory and anti-cancer fields.This paper described the biological function and distribution of BRD4 in human tissues,summarizes the current status of drug development of BRD4 inhibitors,and focuses on the role of BRD4 inhibitors in inflammatory diseases.