走捷径：针对 B 细胞淋巴瘤中的增强子结合锌指蛋白 2。
Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas.
机构信息
Univ. Lille, CHU Lille, ULR 7365 - GRITA - Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France.
Memorial Sloan Kettering Cancer Center, New York, NY, USA.
出版信息
Blood Rev. 2022 Nov;56:100988. doi: 10.1016/j.blre.2022.100988. Epub 2022 Jul 9.
Abstract
Enhancer of zeste homolog 2 (EZH2) is an epigenetic regulator that controls the normal biology of germinal B cells. Overexpression or mutation of EZH2 is associated with malignant transformation in a number of B-cell malignancies; thus, EZH2 inhibitors are an attractive therapeutic option for these targets. Several EZH2 inhibitors have entered clinical trials, but there remains an important question as to how EZH2 inhibitor mechanism of action differs in patients with mutant and wild-type EZH2. This review discusses the EZH2-driven mechanisms that lead to the development of B-cell lymphomas and act as therapeutic targets. Another key area of investigation is whether EZH2 inhibitors will work synergistically with existing immunomodulatory drugs and chemotherapy regimens. In summary, EZH2 inhibitors show potential as treatment for a range of B-cell lymphomas, and numerous clinical evaluations are currently underway.
摘要
EZH2 是一种表观遗传调节剂，可控制生殖 B 细胞的正常生物学功能。EZH2 的过表达或突变与多种 B 细胞恶性肿瘤的恶性转化有关；因此，EZH2 抑制剂是这些靶点的一种有吸引力的治疗选择。几种 EZH2 抑制剂已进入临床试验，但在突变型和野生型 EZH2 患者中，EZH2 抑制剂的作用机制如何存在重要问题。本文讨论了导致 B 细胞淋巴瘤发生并作为治疗靶点的 EZH2 驱动机制。另一个关键研究领域是 EZH2 抑制剂是否会与现有的免疫调节药物和化疗方案协同作用。总之，EZH2 抑制剂显示出治疗一系列 B 细胞淋巴瘤的潜力，目前正在进行大量的临床评估。
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