Herviou Laurie, Cavalli Giacomo, Cartron Guillaume, Klein Bernard, Moreaux Jérôme
Institute of Human Genetics, CNRS UPR1142, Montpellier, France.
University of Montpellier 1, UFR de Médecine, Montpellier, France.
Oncotarget. 2016 Jan 19;7(3):2284-96. doi: 10.18632/oncotarget.6198.
Enhancer of zeste homolog 2 (EZH2), the catalytic subunit of the Polycomb repressive complex 2, inhibits gene expression through methylation on lysine 27 of histone H3. EZH2 regulates normal hematopoietic stem cell self-renewal and differentiation. EZH2 also controls normal B cell differentiation. EZH2 deregulation has been described in many cancer types including hematological malignancies. Specific small molecules have been recently developed to exploit the oncogenic addiction of tumor cells to EZH2. Their therapeutic potential is currently under evaluation. This review summarizes the roles of EZH2 in normal and pathologic hematological processes and recent advances in the development of EZH2 inhibitors for the personalized treatment of patients with hematological malignancies.
zeste 同源物 2 增强子（EZH2）是多梳抑制复合物 2 的催化亚基，通过组蛋白 H3 赖氨酸 27 的甲基化抑制基因表达。EZH2 调节正常造血干细胞的自我更新和分化。EZH2 还控制正常 B 细胞的分化。EZH2 的失调已在包括血液系统恶性肿瘤在内的多种癌症类型中被描述。最近已开发出特异性小分子来利用肿瘤细胞对 EZH2 的致癌依赖性。它们的治疗潜力目前正在评估中。本综述总结了 EZH2 在正常和病理血液学过程中的作用，以及 EZH2 抑制剂开发用于血液系统恶性肿瘤患者个性化治疗的最新进展。
