实用肿瘤学杂志 ›› 2022, Vol. 36 ›› Issue (5): 452-457.doi: 10.11904/j.issn.1002-3070.2022.05.011

• 综述 • 上一篇    下一篇

BCL-2抑制剂在血液恶性肿瘤中的靶向治疗应用及作用机制

何晓晴1, 柯鹏2 综述, 张新友1 审校   

  1. 1.暨南大学第二临床医学院(深圳市人民医院血液内科)(深圳 518000);
    2.苏州大学附属第一医院血液科
  • 收稿日期:2022-01-25 修回日期:2022-09-02 出版日期:2022-10-28 发布日期:2022-11-10
  • 通讯作者: 张新友,E-mail:zxy0518@live.cn
  • 作者简介:何晓晴,女,(1996-),硕士研究生,从事血液肿瘤治疗的研究。
  • 基金资助:
    深圳市科技计划项目(编号:JCYY202103241202100290)

The targeted therapy and mechanism of BCL-2 inhibitor in hematological malignancies

HE Xiaoqing1, KE Peng2, ZHANG Xinyou1   

  1. 1. The Second Clinical Medical College,Jinan University(Department of Hematology,Shenzhen People's Hospital),Shenzhen 518000,China;
    2. Department of Hematology,The First Affiliated Hospital of Soochow University
  • Received:2022-01-25 Revised:2022-09-02 Online:2022-10-28 Published:2022-11-10

摘要: 细胞凋亡受到抑制是血液恶性肿瘤细胞的突出特征。B细胞淋巴瘤-2(B-cell lymphoma-2,BCL-2)是细胞凋亡关键性蛋白调节因子,在多种血液恶性肿瘤中有不同程度的表达。高表达BCL-2的肿瘤细胞抗细胞凋亡能力显著增强,靶向抑制BCL-2成为抗血液肿瘤的研究热点之一。维奈克拉是首个获批上市的BCL-2抑制剂(BCL-2 inhibitor,BCL-2i),用于慢性淋巴细胞白血病、急性髓系白血病及骨髓增生异常综合征的治疗。研究表明维奈克拉对其他血液恶性肿瘤如B细胞非霍奇金淋巴瘤及多发性骨髓瘤也具有抗肿瘤活性。本文就BCL-2抗凋亡机制、BCL-2i在血液恶性肿瘤中的临床应用以及BCL-2i耐药的可能机制作一简要综述。

关键词: B细胞淋巴瘤-2, 细胞凋亡, 维奈克拉, 血液恶性肿瘤

Abstract: Inhibition of apoptosis is a prominent feature of hematological malignancies.B-cell lymphoma-2(BCL-2)is a key protein regulator of apoptosis and is expressed to varying degrees in a variety of hematological malignancies.The anti-apoptotic ability of tumor cells with high expression of BCL-2 is significantly enhanced,and targeted inhibition of BCL-2 has become one of the research hotspots in anti-hematological tumors.Venetoclax(VEN)is the first BCL-2 inhibitor(BCL-2i)approved for the treatment of chronic lymphocytic leukemia,acute myeloid leukemia and myelodysplastic syndromes.Studies have shown that VEN also has antitumor activity against other hematological malignancies such as B-cell non-Hodgkin lymphomas and multiple myeloma.This article briefly reviews the anti-apoptosis mechanism of BCL-2,the clinical application of BCL-2i in hematological malignancies,and the possible mechanism of BCL-2i resistance.

Key words: B-cell lymphoma-2, Apoptosis, Venetoclax, Hematological malignancies

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