lirametostat

Lirametostat (CPI-1205) is an orally available small molecule that acts as a potent and selective inhibitor of the histone lysine methyltransferase Enhancer of zeste homolog 2 (EZH2). It inhibits both wild-type and mutant forms of EZH2, preventing the methylation of histone H3 on lysine 27 (H3K27), which leads to altered gene expression patterns associated with cancer pathways. This results in decreased proliferation of EZH2-expressing cancer cells. EZH2 is a catalytic subunit of the polycomb repressive complex 2 (PRC2) and is often overexpressed or mutated in various cancers, playing a key role in tumor cell proliferation, initiation, progression, stem cell self-renewal, migration, and angiogenesis. Lirametostat has been investigated primarily for its antineoplastic activity in cancers such as prostate cancer and B-cell lymphomas[1][2][4][5][8].

Other names

lirametostat1621862-70-1