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2018 ; 6
(ä): 10
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Epigenetic regulation of cancer progression by EZH2: from biological insights to
therapeutic potential
#MMPMID29556394
Gan L
; Yang Y
; Li Q
; Feng Y
; Liu T
; Guo W
Biomark Res
2018[]; 6
(ä): 10
PMID29556394
show ga
Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase and a catalytic
component of PRC2, catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3)
to regulate gene expression through epigenetic machinery. EZH2 also functions
both as a transcriptional suppressor and a transcriptional co-activator,
depending on H3K27me3 or not and on the different cellular contexts.
Unsurprisingly, numerous studies have highlighted the role of EZH2 in cancer
development and progression. Through modulating critical gene expression, EZH2
promotes cell survival, proliferation, epithelial to mesenchymal, invasion, and
drug resistance of cancer cells. The tumor suppressive effects of EZH2 are also
identified. What is more, EZH2 has decisive roles in immune cells (for example, T
cells, NK cells, dendritic cells and macrophages), which are essential components
in tumor microenvironment. In this review, we aim to discuss the molecular
functions of EZH2, highlight recent findings regarding the physiological
functions and related regulation of EZH2 in cancer pathogenesis. Furthermore, we
summarized and updated the emerging roles of EZH2 in tumor immunity, and current
pre-clinical and clinical trials of EZH2 inhibitors in cancer therapy.