Abstract 3009 Differential Binding Preferences of Histone Trimethyllysine Reader Proteins Offers Promise for Therapeutic Design

Lysine trimethylation (Kme3) is a common post-translational modification (PTM) on histone tails responsible for regulating gene expression, often facilitated via binding of reader proteins. Dozens of human Kme3 reader proteins have been identified, many of which bind to the same histone sequence but have different biological implications. Many readers have been identified as therapeutic targets, but selective inhibition has proven challenging, as these proteins universally bind Kme3 in an aromatic cage.