Highlights•The structure-related regulatory mechanisms of active DNMTs are outlined.•The
therapeutic importance of DNMTs in different cancer types is briefly compared.•The most …

DNA methylation, an epigenetic modification, regulates gene transcription and maintains
genome stability. DNA methyltransferase (DNMT) inhibitors can activate silenced genes at …

Introduction: DNA methylation is an epigenetic modification that modulates gene expression
without altering the DNA base sequence. It plays a crucial role in cancer by silencing tumor …

Epigenetic changes are defined as inherited modifications that are not present in DNA
sequence. Gene expression is regulated at various levels and not only in response to DNA …

The epigenome, which is comprised of chromatin and its associated proteins and the
patterns of covalent modification of DNA by methylation, sets up and maintains gene …

Over the past few years several drugs that target epigenetic modifications have shown
clinical benefits, thus seemingly validating epigenetic cancer therapy. More recently …

Hypermethylation of tumor suppressor genes caused by aberrant activity of DNA
methyltransferases is an important mechanism that contributes to cancer. The reaction …

DNA methylation regulates many cellular processes, including embryonic development,
transcription, chromatin structure, X-chromosome inactivation, genomic imprinting and …

The fundamental role of altered epigenetic modification patterns in tumorigenesis
establishes epigenetic regulatory enzymes as important targets for cancer therapy. Over the …

DNA demethylating agents are approved for some blood malignancies and are under active
investigation in solid tumors, but how these drugs work has remained unclear. In this issue …