Oncogenic roles of enhancer of zeste homolog 1/2 in hematological malignancies

Cancer Science
Makoto Nakagawa, Issay Kitabayashi

Abstract

Polycomb group (PcG) proteins regulate the expression of target genes by modulating histone modifications and are representative epigenetic regulators that maintain the stemness of embryonic and hematopoietic stem cells. Histone methyltransferases enhancer of zeste homolog 1 and 2 (EZH1/2), which are subunits of polycomb repressive complexes (PRC), are recurrently mutated or highly expressed in many hematological malignancies. EZH2 has a dual function in tumorigenesis as an oncogene and tumor suppressor gene, and targeting PRC2, in particular EZH1/2, for anticancer therapy has been extensively developed in the clinical setting. Here, we review the oncogenic function of EZH1/2 and introduce new therapeutic drugs targeting these enzymes.

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Citations

Feb 12, 2020·Biological Chemistry·Stephen L NuttRhys S Allan
Sep 18, 2020·Epigenomics·Ning KangFrancesco Crea
Feb 2, 2019·International Journal of Hematology·Goro SashidaAtsushi Iwama
Oct 2, 2019·Experimental and Therapeutic Medicine·Hao XuWeilin Wang
Mar 8, 2019·Nature Reviews. Endocrinology·Frédéric BrioudeIrene Netchine
Jun 18, 2020·Frontiers in Microbiology·Hiba El HajjOlivier Hermine
May 1, 2021·Biochemical Society Transactions·Christine R Keenan

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Methods Mentioned

BETA
ubiquitination
chemical modifications
transgenic
xenograft
acetylation

Clinical Trials Mentioned

NCT02082977
NCT01897571
NCT02395601
NCT02732275
NCT03110354

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