Elucidating protein–protein interaction (PPI) networks and their structural features within
cells is central to understanding fundamental biology and associations of cell phenotypes …

The discovery of ubiquitin conjugation to lysines and the role of K48-linked polyubiquitin in
targeting substrates for proteasomal degradation was followed by revelation of non …

Abstract DNA methyltransferase 3A (DNMT3A) plays a critical role in establishing and
maintaining DNA methylation patterns in vertebrates. Here we structurally and biochemically …

Protein lysine methyltransferases (PKMTs) transfer up to three methyl groups to the side
chains of lysine residues in proteins and fulfill important regulatory functions by controlling …

Post-translational modification of histones plays a central role in regulating transcription.
Methylation of histone H3 at lysines 4 (H3K4) and 79 (H3K79) play roles in activating …

Hydrogen–deuterium eXchange mass spectrometry (HDX-MS) is increasingly used in drug
development to locate binding sites and to identify allosteric effects in drug/target …

Introduction WDR5 is an epigenetic scaffolding protein that has attracted significant interest
as an anti-cancer drug target, especially in MLL-rearranged leukemias. The most druggable …

Enzymes of the mixed lineage leukemia (MLL) family of histone H3 lysine 4 (H3K4)
methyltransferases are critical for cellular differentiation and development and are regulated …

Site-selective conjugation chemistry has proven effective to synthesize homogenously
ubiquitinated histones. Recently, a powerful strategy using 2-((2-chloroethyl) amino) ethane …

Enzymes that regulate the degree of histone H3 lysine 4 (H3K4) methylation are crucial for
proper cellular differentiation and are frequently mutated in cancer. The Mixed lineage …