Targeting histone methyltransferase EZH2 as cancer treatment.

摘要: It is widely accepted that epigenetic alterations are associated with different stages of tumour formation and progression in many cancers. Therefore, abnormalities cancers emerging as important biomarkers may have therapeutic potential. The polycomb repressive complex 2 (PRC2) a key regulator catalyses trimethylation lysine 27 on histone H3 (H3K27me3) via the methyltransferase, EZH2, which confers stemness regulates differentiation during embryonic development. Given these roles EZH2 H3K27me3, plastic dynamic features cancer cells, especially stem cells (CSCs), be closely this mechanism. In addition, recent sequencing technology revealed there recurrent mutations polycomb-related genes, including types researchers focused targeting novel treatment identified small compounds inhibit activity. Some them now under clinical trial B-cell lymphoma. However, underlying mechanisms by PRC2 precisely regulate at certain genomic loci cellular conditions remain unclear. review, I focus advancements research, its regulation CSC population, discuss perspectives challenges for near future.