Histone modifications are key epigenetic regulatory features that have important roles in
many cellular events. Lysine methylations mark various sites on the tail and globular …

Cancer arises from genetic alterations that invariably lead to dysregulated transcriptional
programs. These dysregulated programs can cause cancer cells to become highly …

Chromosomal rearrangements of the human MLL/KMT2A gene are associated with infant,
pediatric, adult and therapy-induced acute leukemias. Here we present the data obtained …

Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …

Histone posttranslational modifications represent a versatile set of epigenetic marks
involved not only in dynamic cellular processes, such as transcription and DNA repair, but …

Abstract Pinometostat (EPZ-5676) is a first-in-class small-molecule inhibitor of the histone
methyltransferase disrupter of telomeric silencing 1-like (DOT1L). In this phase 1 study …

Ubiquitination-dependent histone crosstalk plays critical roles in chromatin-associated
processes and is highly associated with human diseases. Mechanism studies of the …

The DNA of each cell is wrapped around histone octamers, forming so-called 'nucleosomal
core particles'. These histone proteins have tails that project from the nucleosome and many …

Inhibition of the Menin (MEN1) and MLL (MLL1, KMT2A) interaction is a potential therapeutic
strategy for MLL-rearranged (MLL-r) leukemia. Structure-based design yielded the potent …

The mixed-lineage leukemia 1 (MLL1) gene (now renamed Lysine [K]-specific
MethylTransferase 2A or KMT2A) on chromosome 11q23 is disrupted in a unique group of …