EZH2 in normal hematopoiesis and hematological malignancies

被引:80
|
作者
Herviou, Laurie [2 ]
Cavalli, Giacomo [2 ]
Cartron, Guillaume [3 ,4 ]
Klein, Bernard [1 ,2 ,3 ]
Moreaux, Jerome [1 ,2 ,3 ]
机构
[1] CHU Montpellier, Dept Biol Hematol, Montpellier, France
[2] CNRS, Inst Human Genet, UPR1142, Montpellier, France
[3] Univ Montpellier I, UFR Med, Montpellier, France
[4] CHU Montpellier, Dept Clin Hematol, Montpellier, France
关键词
hematological malignancies; EZH2; Polycomb complex; therapeutic target; HISTONE METHYLTRANSFERASE EZH2; POLYCOMB-GROUP GENE; GROUP PROTEIN EZH2; B-CELL LYMPHOMAS; AGGRESSIVE BREAST-CANCER; REPRESSIVE COMPLEX 2; GERMINAL-CENTER; SOMATIC MUTATIONS; STEM-CELLS; SELECTIVE-INHIBITION;
D O I
10.18632/oncotarget.6198
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
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.
引用
收藏
页码:2284 / 2296
页数:13
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