Epigenetic alternations concern heritable yet reversible changes in histone or DNA
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …

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 …

The implementation of targeted therapies for acute myeloid leukaemia (AML) has been
challenging because of the complex mutational patterns within and across patients as well …

FTO, an mRNA N 6-methyladenosine (m 6 A) demethylase, was reported to promote
leukemogenesis. Using structure-based rational design, we have developed two promising …

Metabolic rewiring and epigenetic remodeling, which are closely linked and reciprocally
regulate each other, are among the well-known cancer hallmarks. Recent evidence …

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 …

Next-generation sequencing has revealed that more than 50% of human cancers harbour
mutations in enzymes that are involved in chromatin organization. Tumour cells not only are …

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' …

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 …

Cyclobutanes are increasingly used in medicinal chemistry in the search for relevant
biological properties. Important characteristics of the cyclobutane ring include its unique …