EZH2 Degraders Small Molecules and Peptides

Enhancer of zeste homolog 2 (EZH2) EC 2.1.1.43 is a lysine methyltransferase that catalyses the transfer of methyl groups from S-adenosylmethionine (SAM) to histone H3 at lysine 27. This facilitates the formation of heterochromatin and regulates gene expression.

EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) complex which regulates cell fate. Methylation of H3 by the complex leads to silencing of target genes involved in cell cycle regulation, cell proliferation, ...