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DNA (cytosine-5)-methyltransferase 1, DNA (cytosine-5)-methyltransferase 3A, DNA (cytosine-5)-methyltransferase 3B (DNMT1, DNMT3A, DNMT3B)

Target
DNMT1, DNMT3A, DNMT3B
Molecular classification
Enzyme, Epigenetic regulator, DNA methyltransferase
01

Overview

DNA (cytosine-5)-methyltransferase 1 (DNMT1) and its paralogs DNMT3A and DNMT3B are enzymes that catalyze the transfer of methyl groups to cytosine residues in DNA, predominantly at CpG dinucleotides, resulting in DNA methylation[1][2][3]. DNMT1 is primarily responsible for maintenance methylation after DNA replication, ensuring the faithful inheritance of epigenetic marks, while DNMT3A and DNMT3B are primarily involved in de novo DNA methylation during development[1][3]. Aberrant activity or expression of these enzymes is implicated in various human disorders, most notably cancer, where altered methylation patterns can lead to inappropriate gene silencing[2][3]. Drugs targeting DNMTs, such as azacitidine and decitabine, are used in the treatment of certain leukemias and myelodysplastic syndromes, working by inhibiting DNMT activity and thereby reversing abnormal gene silencing[2][3]. DNMT1, DNMT3A, and DNMT3B are major regulators of epigenetic programming and play essential roles in cellular differentiation, genomic imprinting, X-chromosome inactivation, and suppression of transposable elements[1][2][3].

Other names
CXXC finger protein 9CXXC-type zinc finger protein 9CXXC9DNA methyltransferase HsaIHSN1EMCMTAIMDNMT1_HUMANDNA (cytosine-5-)-methyltransferase 1DNA MTase HsaIm.HsaIDNA (cytosine-5)-methyltransferase 3 alphaDNMT3A_HUMANDNA (cytosine-5)-methyltransferase 3 betaDNMT3B_HUMAN
02

Mechanism of action

Inhibition of DNA methyltransferase activity, leading to DNA hypomethylation and reactivation of silenced tumor suppressor genes

03

Biological functions

DNA methylationEpigenetic regulationGene silencingRegulation of transcriptionCell differentiationMaintenance of genomic stabilityNeurodevelopment
04

Disease associations

CancerNeurodegenerative diseaseDevelopmental disordersHereditary sensory neuropathy
05

Safety considerations

MyelosuppressionDNA damage and mutagenesisOff-target effects leading to global demethylation and activation of oncogenes
06

Interacting drugs

Azacitidine

3 more in the full profile.

07

Biomarkers

DNA methylation status (e.g., global or gene-specific methylation patterns)DNMT1 expression level

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