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

2018; Wiley; Volume: 109; Issue: 8 Linguagem: Inglês

10.1111/cas.13655

1349-7006

Makoto Nakagawa, Issay Kitabayashi,

Cancer-related gene regulation

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 ( EZH 1/2), which are subunits of polycomb repressive complexes ( PRC ), are recurrently mutated or highly expressed in many hematological malignancies. EZH 2 has a dual function in tumorigenesis as an oncogene and tumor suppressor gene, and targeting PRC 2, in particular EZH 1/2, for anticancer therapy has been extensively developed in the clinical setting. Here, we review the oncogenic function of EZH 1/2 and introduce new therapeutic drugs targeting these enzymes.