Abstract Histone–lysine N-methyltransferase 2 (KMT2) family proteins methylate lysine 4 on
the histone H3 tail at important regulatory regions in the genome and thereby impart crucial …

Antagonism of protein–protein interactions (PPIs) with small molecules is becoming more
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …

Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Activation of oncogenes or the deactivation of tumor suppressor genes has long been
established as the fundamental mechanism leading towards carcinogenesis. Although this …

MYC is an oncoprotein transcription factor that is overexpressed in the majority of
malignancies. The oncogenic potential of MYC stems from its ability to bind regulatory …

Protein arginine methyltransferases (PRMTs) play important roles in several cellular
processes, including signaling, gene regulation, and transport of proteins and nucleic acids …

SET domain-containing proteins belong to a group of enzymes named after a common
domain that utilizes the cofactor S-adenosyl-L-methionine (SAM) to achieve methylation of …

The WDR5 subunit of the MLL complex enforces active chromatin and can bind RNA; the
relationship between these two activities is unclear. Here we identify a RNA binding pocket …

Methylation of histone H3K4 is a hallmark of actively transcribed genes that depends on
mono-ubiquitination of histone H2B (H2B-Ub). H3K4 methylation in yeast is catalyzed by …

Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …