Target type: molecularfunction
Catalysis of the reaction: L-lysyl9-[histone H3] + S-adenosyl-L-methionine = H+ + N6-methyl-L-lysyl9-[histone H3] + S-adenosyl-L-homocysteine. This reaction is the addition of a methyl group to the unmethylated lysine residue at position 9 of histone H3, producing histone H3K9me. [RHEA:60288]
Histone H3K9 monomethyltransferase activity catalyzes the transfer of a single methyl group from a donor molecule, typically S-adenosyl-L-methionine (SAM), to the lysine 9 residue of histone H3. This methylation event is a crucial epigenetic modification that plays a vital role in regulating gene expression and chromatin structure.
The enzyme specifically recognizes and binds to the histone H3 tail, specifically targeting lysine 9 (K9) for methylation. The methylation process is highly regulated and influenced by various factors, including the presence of other histone modifications, DNA sequence context, and cellular signaling pathways.
H3K9 methylation can lead to the formation of heterochromatin, a tightly packed chromatin structure that is generally associated with gene silencing. Methylated H3K9 serves as a docking site for proteins containing chromodomains, such as HP1 (Heterochromatin Protein 1). These proteins bind to methylated H3K9, further stabilizing the heterochromatin structure and promoting gene repression.
In addition to gene silencing, H3K9 methylation is implicated in a wide range of cellular processes, including DNA replication, DNA repair, and chromosome stability. Aberrant H3K9 methylation has been linked to various human diseases, including cancer and developmental disorders.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Histone-lysine N-methyltransferase SETDB1 | A histone-lysine N-methyltransferase SETDB1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15047] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| s-adenosylhomocysteine | S-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 |
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source |