oral, allosteric PRC2 inhibitor (EED) - Novartis, Emeryville, CA

oral, allosteric PRC2 inhibitor (EED)

in Ph. I/II for cancer (DLBCL); preliminary efficacy

from micromolar HTS hit

J. Med. Chem.

Novartis, Emeryville, CA

Context. MAK683 is an oral, allosteric and selective PRC2 inhibitor intended for PRC2-dependent cancers. PRC2 is an essential epigenetic regulator of gene expression and enhanced or diminished PRC2 function…

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