Lysine Methyltransferases

Lysine methyltransferases are enyzmes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones, particularly histones H3 and H4. The dysregulation of this methylation is critical in the development of cancer.

Targets
Literature
Receptor Data

Lysine Methyltransferase Target Files

Lysine methyltransferases, or KMTs, are enzymes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones. Upward of 24 human protein lysine methyltransferases have been described and they belong to the histone methyltransferase group of enzymes, which also includes protein arginine methyltransferases. They are also closely related in biological activity to the DNA methyltransferases.

Histones represent the major protein component of chromatin, around which DNA is coiled within the nucleus. Modification of histone protein by methylation induces chromatin remodeling which in turn alters gene expression. Histone methylation is an integral epigenetic process during development and represents an important mechanism of transcriptional regulation and chromatin remodeling. Dysregulation of histone methylation has been implicated in diseases including cancer.

Histone methylation by KMTs occurs predominantly on lysine residues in histones H3 and H4, and multiple methyl groups may be added to each residue.The epigenetic effects of histone methylation are dependent on the residue undergoing methylation and the degree of methylation. Consequently different types of lysine methylation are associated with different functions in the regulation of gene expression. Lysine methylation can induce both transcriptional activation and silencing.

Literature for Lysine 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
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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.

Lysine Methyltransferase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Euchromatic histone-lysine N-methyltransferase 1 (GLP) Human EHMT1 NM_024757 Q9H9B1
Mouse Ehmt1 NM_001012518 Q5DW34
Rat Ehmt1 NM_001108572 NP_001102042
Euchromatic histone-lysine N-methyltransferase 2 (G9a) Human EHMT2 NM_006709 Q96KQ7
Mouse Ehmt2 NM_145830 Q9Z148
Rat Ehmt2 NM_212463 NP_997628
SET domain containing 2 Human SETD2 NM_014159 Q9BYW2
Mouse Setd2 NM_001081340 E9Q5F9
Rat Setd2 NM_001108189 NP_001101659
SET domain containing (lysine methyltransferase) 7 (SET9) Human SETD7 NM_030648 Q8WTS6
Mouse Setd7 NM_080793 Q8VHL1
Rat Setd7 NM_001109558 NP_001103028
SET domain containing (lysine methyltransferase) 8 Human SETD8 NM_020382 Q9NQR1
Mouse Setd8 NM_001310723 Q2YDW7
Rat Setd8 NM_001246665 NP_001233594
SET domain, bifurcated 1 Human SETDB1 NM_001145415 Q15047
Mouse Setdb1 NM_001163641 O88974
Rat Setdb1 XM_002726023 NP_001258104
SET domain, bifurcated 2 Human SETDB2 NM_031915 Q96T68
Mouse Setdb2 NM_001081024 Q8C267
Rat Setdb2 XM_224248 XP_224248
SET domain containing 1A Human SETD1A NM_014712 O15047
Mouse Setd1a NM_178029 Q80V17
Rat - - -
SET domain containing 1B Human SETD1B XM_037523 Q9UPS6
Mouse Setd1b NM_001040398 Q8CFT2
Rat Setd1b XM_219358 XP_219358
Nuclear receptor binding SET protein domain 1 Human NSD1 NM_172349 Q96L73
Mouse Nsd1 NM_008739 O88491
Rat Nsd1 NM_00107337 NP_001100807
SET and MYND domain containing 2 Human SMYD2 NM_020197 Q9NRG4
Mouse Smyd2 NM_026796 Q8R5A0
Rat Smyd2 NM_206851 Q7M6Z3
PR domain containing 2m with ZNF domain Human PRDM2 NM_012231 Q13029
Mouse Prdm2 NM_001081355 A2A7B5
Rat Prdm2 NM_001077648 Q63755