Enhancer of Zeste Homolog 2 (EZH2) is the core component of the polycomb repressive
complex 2 (PRC2), possessing the enzymatic activity in generating di/tri-methylated lysine 27 in histone
H3. EZH2 has important roles during early development, and its dysregulation is heavily linked to
oncogenesis in various tissue types. Accumulating evidences suggest a remarkable therapeutic potential
by targeting EZH2 in cancer cells. The first part reviews current strategies to target EZH2 in cancers,
and evaluates the available compounds and agents used to disrupt EZH2 functions. Then we provide insight to the
future direction of the research on targeting EZH2 in different cancer types. We comprehensively discuss the current understandings
of the 1) structure and biological activity of EZH2, 2) its role during the assembling of PRC2 and recruitment
of other protein components, 3) the molecular events directing EZH2 to target genomic regions, and 4) post-translational
modification at EZH2 protein. The discussion provides the basis to inspire the development of novel strategies to abolish
EZH2-related effects in cancer cells.
Keywords: Chemotherapy, DNA methylation, DZNep, EZH2, H3K27me3, LncRNA, PRC2, SET domain.
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