Target intelligence / Profile preview

DNA Methylome (DNAm)

Target
DNAm
Molecular classification
DNA modification, Other
01

Overview

The DNA methylome refers to the comprehensive set of cytosine methylation modifications across the entire genome of a cell [1]. It primarily involves the addition of a methyl group to the 5-carbon of cytosine residues within CpG dinucleotides, serving as a fundamental epigenetic mechanism for controlling gene expression [2]. High levels of methylation in promoter regions typically correlate with transcriptional silencing, which is essential for normal development, genomic imprinting, and X-chromosome inactivation [2]. In pathological states, particularly oncology, the methylome often undergoes massive reorganization characterized by global hypomethylation and focal hypermethylation of tumor suppressor genes [3]. While the methylome itself is a genomic state rather than a single protein target, it is therapeutically modulated using DNA methyltransferase (DNMT) inhibitors like azacitidine and decitabine to reverse aberrant silencing [4]. These drugs incorporate into DNA and trap DNMT enzymes, resulting in a loss of methylation during subsequent rounds of cell division [4].

Other names
DNA methylation landscapeGenomic methylation patternEpigenome (DNA methylation component)
02

Mechanism of action

Inhibition of DNA methyltransferases (DNMTs), leading to global DNA hypomethylation and the reactivation of epigenetically silenced genes [4].

03

Biological functions

Gene silencingGenomic imprintingX-chromosome inactivationChromatin structure regulationCellular differentiationOther
04

Disease associations

CancerHematologic malignancyNeurodevelopmental disorderAgingInflammationOther
05

Safety considerations

MyelosuppressionNon-specific gene activationGenomic instabilityCytotoxicity
06

Interacting drugs

Azacitidine

3 more in the full profile.

07

Biomarkers

MGMT promoter methylationSEPT9 methylationGSTP1 methylationDNAmAge (Epigenetic clock)

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