Function
Histone methyltransferase (HMT) are histone-lysine N-methyltransferase (KHMT) and histone-arginine N-methyltransferase (RHMT) which catalyzes the transfer of methyl groups to lysine and arginine residues of histones[1]. HMT use S-adenosyl methionine (SAM) or S-adenosyl homocysteine (SAH) as the methyl donor. KHMT can be SET domain-containing or non-SET domain-containing. The SET domain contains the catalytic core of KHMT and targets the lysine tail region of KHMT. CxxC domain is a zinc finger domain.
For SET7/9 see Histone Lysine Methyltransferase SET7/9.
- euchromatin histone methyltransferase dimethylates histone H3 at Lys 9 resulting in transcriptional repression[2].
- DOT1L histone methyltransferase methylates histone H3 at Lys 79 resulting in transcriptional repression[3].
Relevance
Inhibitors of the histone-lysine N-methyltransferase SMYD2 which represses the tumor-suppressing activities of p53 are studied as cancer therapy drugs[4].
Disease
Aberrant HMT plays a role in cancer, intellectual disability syndromes and regulation of tissue aging[5].
Structural highlights
Human inserted in a hydrophobic environment[6]. Water molecules shown as red spheres
3D Structures of histone methyltransferase
Histone methyltransferase 3D structures
