Page last updated: 2024-10-24

lysine N-methyltransferase activity

Definition

Target type: molecularfunction

Catalysis of the transfer of a methyl group from S-adenosyl-L-methionine to the epsilon-amino group of a lysine residue. [GOC:mah]

Lysine N-methyltransferase activity is a crucial enzymatic function involved in the post-translational modification of proteins. This process entails the transfer of a methyl group from a methyl donor, typically S-adenosyl methionine (SAM), to the ε-amino group of a lysine residue within a target protein. This methylation event can significantly alter the protein's structure, function, and interactions with other molecules. The specific outcome of lysine methylation is highly dependent on the target protein, the location of the modified lysine residue, and the number of methyl groups added (mono-, di-, or tri-methylation). Lysine N-methyltransferases play a pivotal role in a wide range of cellular processes, including:

- **Gene regulation**: Methylation of histones, the proteins that package DNA, can alter chromatin structure and influence gene expression. This regulation can involve both activation and repression of gene transcription.
- **Signal transduction**: Methylation events can modify the activity of signaling proteins, influencing cellular responses to various stimuli.
- **Cellular metabolism**: Lysine methylation can regulate metabolic pathways by affecting the activity of enzymes involved in these pathways.
- **Protein stability and degradation**: Methylation can influence protein stability and degradation by affecting their interactions with other proteins, such as ubiquitin ligases, which mediate protein breakdown.
- **Immune response**: Methylation plays a role in the regulation of the immune system, influencing the activation and function of immune cells.

Dysregulation of lysine N-methyltransferase activity has been linked to various human diseases, including cancer, neurodevelopmental disorders, and autoimmune diseases. Therefore, understanding the intricate mechanisms of lysine methylation is crucial for developing novel therapeutic strategies targeting these conditions.'
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Proteins (4)

ProteinDefinitionTaxonomy
N-lysine methyltransferase SMYD2An N-lysine methyltransferase SMYD2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NRG4]Homo sapiens (human)
N-lysine methyltransferase KMT5AAn N-lysine methyltransferase KMT5A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NQR1]Homo sapiens (human)
N-lysine methyltransferase SMYD2An N-lysine methyltransferase SMYD2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NRG4]Homo sapiens (human)
N-lysine methyltransferase KMT5AAn N-lysine methyltransferase KMT5A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NQR1]Homo sapiens (human)

Compounds (8)

CompoundDefinitionClassesRoles
nsc 663284NSC 663284: structure in first sourcequinolone
s-adenosylhomocysteineS-adenosyl-L-homocysteine : An organic sulfide that is the S-adenosyl derivative of L-homocysteine.

S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions.
adenosines;
amino acid zwitterion;
homocysteine derivative;
homocysteines;
organic sulfide
cofactor;
EC 2.1.1.72 [site-specific DNA-methyltransferase (adenine-specific)] inhibitor;
EC 2.1.1.79 (cyclopropane-fatty-acyl-phospholipid synthase) inhibitor;
epitope;
fundamental metabolite
2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dioneaminotoluene
bvt.948
az 505AZ 505: an SMYD2 inhibitor; structure in first source
unc 03217-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine: a G9a antagonist; structure in first sourcequinazolines
6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source
lly-507LLY-507 : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl}[biphenyl]-3-carboxylic acid with the amino group of 3-(pyrrolidin-1-yl)propan-1-amine. It is a potent and selective inhibitor of SMYD2 and inhibits the ability of SMYD2 to methylate p53. It serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.

LLY-507: inhibits methyltransferase SMYD2; structure in first source