Target type: molecularfunction
Catalysis of the reaction: L-lysyl36-[histone H3] + 2 S-adenosyl-L-methionine = 2 H+ + N6,N6-dimethyl-L-lysyl36-[histone H3] + 2 S-adenosyl-L-homocysteine. This reaction is the successive addition of two methyl groups to the lysine residue at position 36 of histone H3, producing histone H3K36me2. [RHEA:60308]
Histone H3K36 dimethyltransferase activity refers to the enzymatic ability to catalyze the transfer of two methyl groups from a donor molecule, typically S-adenosyl methionine (SAM), to the lysine residue at position 36 of histone H3. This methylation event is a crucial post-translational modification (PTM) that plays a vital role in regulating various cellular processes, including gene expression, DNA replication, and repair.
The methylation of histone H3 at lysine 36 (H3K36me2) is generally associated with actively transcribed regions of the genome. The presence of this mark serves as a signal for the recruitment of various protein complexes involved in gene transcription, including histone acetyltransferases (HATs) and elongation factors. These factors facilitate the unwinding of DNA, making it accessible for RNA polymerase and promoting the elongation of transcripts.
Furthermore, H3K36me2 has been implicated in the prevention of aberrant transcription initiation within coding regions. This is achieved through its interaction with factors like the Set2/Rpd3S complex, which can suppress the activity of transcription initiation factors and promote the recruitment of histone deacetylases (HDACs) to silence spurious transcription.
Overall, the molecular function of histone H3K36 dimethyltransferase activity is multifaceted, impacting gene expression, DNA replication, and repair. It acts as a critical regulator of chromatin structure and function, influencing both the initiation and elongation phases of transcription. The precise role of H3K36me2 in these processes is context-dependent and can vary depending on the specific cellular context and the interplay with other chromatin modifications.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Histone-lysine N-methyltransferase SMYD3 | A histone-lysine N-methyltransferase SMYD3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H7B4] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase SETMAR | A histone-lysine N-methyltransferase SETMAR that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q53H47] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase NSD2 | A histone-lysine N-methyltransferase NSD2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O96028] | 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 |
| scutellarein | scutellarein : Flavone substituted with hydroxy groups at C-4', -5, -6 and -7. scutellarein: aglycone of scutellarin from Scutellaria baicalensis; carthamidin is 2S isomer of scutellarein; do not confuse with isoscutellarein and/or isocarthamidin which are respective regioisomers, or with the scutelarin protein | tetrahydroxyflavone | metabolite |
| az 505 | AZ 505: an SMYD2 inhibitor; structure in first source | ||
| gsk343 | GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). GSK343: an EZH2 methyltransferase inhibitor | aminopyridine; indazoles; N-alkylpiperazine; N-arylpiperazine; pyridone; secondary carboxamide | antineoplastic agent; apoptosis inducer; EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor |