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[BRD4及其抑制剂在血液系统恶性肿瘤中的作用机制研究进展——综述]

[Research Advances in the Mechanisms of BRD4 and Its Inhibitors in Hematologic Malignancies--Review].

作者信息

Gao Ri-Li, Zeng Cheng-Wu, Li Yang-Qiu

机构信息

Key Laboratory for Regenerative Medicine of Ministry of Education, Institute of Hematology, School of Medicine, Jinan University, Guangzhou 510632, Guangdong Province, China.

Key Laboratory for Regenerative Medicine of Ministry of Education, Institute of Hematology, School of Medicine, Jinan University, Guangzhou 510632, Guangdong Province, China,E-mail:

出版信息

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2021 Aug;29(4):1365-1368. doi: 10.19746/j.cnki.issn.1009-2137.2021.04.057.

Abstract

Bromodomain-containing protein 4 (BRD4) is one of the most important members in the bromodomain and extra terminal domain(BET) family, it plays an important role in cellular physiology in human body, such as cell cycles, cell proliferation, and immune response. Recent studies have shown that BRD4 is associated with occurrence and development of acute myeloblastic leukemia, multiple myeloma and lymphoma. The mechanisms of BRD4 in hematologic malignancies including the regulation of c-Myc expression, and participation of the composition of super-enhancer, etc. At present, many kinds of inhibitors have been developed to target inhibit BRD4 for therapy in hematologic malignancies, and some of BRD4 inhibitors have entered phase Ⅱ clinical trials, which suggested that BRD4 inhibitors are expected to become new therapeutic agents for hematologic malignancies. In this review, the research advance of BRD4 and BRD4 inhibitors in hematologic malignancies was summarized briefly.

摘要

含溴结构域蛋白4(BRD4)是溴结构域和额外末端结构域(BET)家族中最重要的成员之一,它在人体细胞生理过程中发挥着重要作用,如细胞周期、细胞增殖和免疫反应。最近的研究表明,BRD4与急性髓细胞白血病、多发性骨髓瘤和淋巴瘤的发生发展有关。BRD4在血液系统恶性肿瘤中的作用机制包括对c-Myc表达的调控以及参与超级增强子的组成等。目前,已经开发出多种靶向抑制BRD4的抑制剂用于血液系统恶性肿瘤的治疗,部分BRD4抑制剂已进入Ⅱ期临床试验,这表明BRD4抑制剂有望成为血液系统恶性肿瘤的新型治疗药物。本文简要综述了BRD4及其抑制剂在血液系统恶性肿瘤中的研究进展。

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