Target type: molecularfunction
Catalysis of the reaction: S-adenosyl-L-methionine + (histone H3)-arginine (position 2) = S-adenosyl-L-homocysteine + (histone H3)-N-methyl-arginine (position 2). This reaction is the addition of a methyl group to the arginine residue at position 2 of histone H3. [GOC:mah, PMID:17898714]
Histone H3R2 methyltransferase activity refers to the enzymatic ability to catalyze the transfer of a methyl group from a donor molecule, such as S-adenosyl methionine (SAM), to the arginine residue at position 2 (R2) of histone H3. This methylation event is a critical epigenetic modification that plays a crucial role in regulating gene expression. Histone H3R2 methylation is associated with various cellular processes, including DNA replication, transcription, and chromatin remodeling. The specific effect of methylation at this site can vary depending on the degree of methylation (mono-, di-, or tri-methylation) and the cellular context. For example, mono-methylation of H3R2 has been linked to transcriptional activation, while di-methylation has been associated with transcriptional repression. The enzymes responsible for catalyzing this methylation reaction are known as histone H3R2 methyltransferases (H3R2MTs), which belong to a larger family of enzymes called histone lysine methyltransferases (HKMTs). These enzymes typically contain a conserved SET domain, which is responsible for the catalytic activity. H3R2MTs are often targeted by regulatory proteins and signaling pathways, highlighting the importance of this epigenetic mark in controlling gene expression. Aberrant methylation of H3R2 has been implicated in various diseases, including cancer, suggesting that H3R2MTs could be potential therapeutic targets.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Protein arginine N-methyltransferase 6 | A protein arginine N-methyltransferase 6 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96LA8] | Homo sapiens (human) |
| Histone-arginine methyltransferase CARM1 | A histone-arginine methyltransferase CARM1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q86X55] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| sulfathiazole | sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine. | 1,3-thiazoles; substituted aniline; sulfonamide; sulfonamide antibiotic | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| c.i. direct red 23 | C.I. Direct Red 23: azo dye; structure in first source | ||
| furamidine | furamidine: RN given refers to parent cpd; WR 199385 refers to di-HCl; pafuramidine is a prodrug of this | ||
| 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 |
| stilbamidine | stilbamidine: RN given refers to parent cpd | ||
| 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 |