DNA Methyltransferases

DNA methyltransferases (DNMTs) are a family of enzymes that catalyze the addition of methyl groups onto DNA. The mechanism of action involves the transfer of a methyl group from S-adenosyl methionine (SAM) to the target DNA.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
3842 5-Azacytidine
DNA methyltransferase inhibitor
2624 Decitabine
DNA methyltransferase inhibitor
4524 EGCG
DNMT1 inhibitor
5016 Fisetin
DNMT1 inhibitor
4359 Lomeguatrib
MGMT inhibitor
3295 RG 108
Non-nucleoside DNA methyltransferase inhibitor
5155 SGI 1027
DNA methyltransferase inhibitor
2293 Zebularine
DNA methyltransferase and cytidine deaminase inhibitor

Other

Cat No Product Name / Activity
1745 5-Iodotubercidin
Potent adenosine kinase inhibitor; decreases DNA methylation
4061 6-Thioguanine
Anticancer and immunosuppressive agent; disrupts cytosine methylation

DNA methyltransferases (DNMTs) are a family of enzymes that catalyze the addition of methyl groups onto DNA. The mechanism of action involves the transfer of a methyl group from S-adenosyl methionine (SAM) to the target DNA; this is similar to the mechanism employed by histone methyltransferases.

DNA methylation is an epigenetic mechanism that alters protein expression. DNA methylation commonly occurs at sites known as "CpG islands" - these are genomic areas rich in cytosine and guanine nucleotide base pairs that are often present near or at the promoter region of a gene. Methylation of cytosine residues can prevent transcription factor binding, thereby directly inhibiting transcription. DNA methylation also prompts the recruitment of methyl-CpG-binding proteins which indirectly inhibit transcription through chromatin remodeling. In addition to CpG islands, areas of DNA proximal to these islands - termed "CpG shores" - are also 'hotspots' for DNA methylation.

DNMTs can be classified according to their target nucleotide. The most common form of DNA methylation occurs on cytosine nucleotides, generating C5-methylcytosine, though lower eukaryotes and prokaryotes also express enzymes that generate N6-methyladenine and N4-methylcytosine. DNA methylation also occurs on guanine nucleotides through the biological activity of MGMT. Dysregulation of DNA methylation has been implicated in diseases including cancer, where hypomethylation of oncogenes and hypermethylation of tumor suppressor genes occurring in cancer cell lines is thought to promote tumorigenesis.

Literature for DNA Methyltransferases

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases

DNA Methyltransferase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
DNA (cytosine-5-)-methyltransferase 1 Human DNMT1 NM_001379 P26358
Mouse Dnmt1 NM_001199433 P13864
Rat Dnmt1 NM_053354 Q9Z330
DNA (cytosine-5-)-methyltransferase 3 α Human DNMT3A NM_022552 Q9Y6K1
Mouse Dnmt3a NM_007872 O88508
Rat Dnmt3a NM_001003957 Q5FVL1
DNA (cytosine-5-)-methyltransferase 3 β Human DNMT3B NM_006892 Q9UBC3
Mouse Dnmt3b NM_001003961 O88509
Rat Dnmt3b NM_001003959 Q1LZ51
O-6-methylguanine-DNA methyltransferase Human MGMT NM_002412 P16455
Mouse Mgmt NM_008598 P26187
Rat Mgmt NM_012861 P24528