Article
Structure of the catalytic domain of EZH2 reveals conformational plasticity in cofactor and substrate binding sites and explains oncogenic mutations.
PloS one - 1 Jan 2013
Wu Hong, Zeng Hong, Dong Aiping, Li Fengling, He Hao, Senisterra Guillermo, Seitova Alma, Duan Shili, Brown Peter J, Vedadi Masoud, Arrowsmith Cheryl H, Schapira Matthieu
Abstract excerpt
Polycomb repressive complex 2 (PRC2) is an important regulator of cellular differentiation and cell type identity. Overexpression or activating mutations of EZH2, the catalytic component of the PRC2 complex, are linked to hyper-trimethylation of lysine 27 of histone H3 (H3K27me3) in many cancers. Potent EZH2 inhibitors that reduce levels of H3K27me3 kill mutant lymphoma cells and are efficacious in a mouse...
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