EZH2 in normal hematopoiesis and hematological malignancies
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Laurie Herviou2, Giacomo Cavalli2, Guillaume Cartron3,4, Bernard Klein1,2,3 and Jérôme Moreaux1,2,3
1 Department of Biological Hematology, CHU Montpellier, Montpellier, France
2 Institute of Human Genetics, CNRS UPR1142, Montpellier, France
3 University of Montpellier 1, UFR de Médecine, Montpellier, France
4 Department of Clinical Hematology, CHU Montpellier, Montpellier, France
Jérôme Moreaux, email:
Keywords: hematological malignancies, EZH2, Polycomb complex, therapeutic target
Received: August 07, 2015 Accepted: October 14, 2015 Published: October 20, 2015
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.
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