Target type: molecularfunction
Catalysis of the reaction: S-adenosyl-L-methionine + (histone)-arginine = S-adenosyl-L-homocysteine + (histone)-N-methyl-arginine. [PMID:8002954]
Histone arginine N-methyltransferases (PRMTs) are a family of enzymes that catalyze the transfer of a methyl group from S-adenosyl-L-methionine (SAM) to the guanidino nitrogen of arginine residues in histone proteins. This process is known as methylation and is a key epigenetic modification that regulates gene expression. PRMTs play a critical role in a variety of cellular processes, including transcription, DNA replication, and cell cycle progression. They are highly specific for arginine residues within histone tails, and their activity is often influenced by the presence of other histone modifications and by the specific sequence context of the target arginine. The methylation of histone arginine residues can have a variety of effects on gene expression, depending on the specific site and the degree of methylation. For example, methylation of histone H4 arginine 3 (H4R3) can activate gene transcription, while methylation of histone H3 arginine 17 (H3R17) can repress gene transcription. PRMTs also play a role in the regulation of other cellular processes, such as DNA replication and repair. The activity of PRMTs is regulated by a variety of factors, including the availability of SAM, the presence of other histone modifications, and the specific sequence context of the target arginine. They are also subject to regulation by other enzymes, such as kinases and phosphatases. The dysregulation of PRMT activity has been linked to various diseases, including cancer, autoimmune diseases, and neurodegenerative disorders. '
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Protein | Definition | Taxonomy |
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Protein arginine N-methyltransferase 5 | A protein arginine N-methyltransferase 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O14744] | Homo sapiens (human) |
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 |
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pentamidine | pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
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 |
s-adenosylmethionine | acylcarnitine: structure in first source S-adenosyl-L-methioninate : A sulfonium betaine that is a conjugate base of S-adenosyl-L-methionine obtained by the deprotonation of the carboxy group. | sulfonium betaine | human metabolite |
hexamidine | hexamidine : A polyether that is the bis(4-guanidinophenyl) ether of hexane-1,6-diol. | aromatic ether; guanidines; polyether | antimicrobial agent; antiseptic drug |
sinefungin | adenosines; non-proteinogenic alpha-amino acid | antifungal agent; antimicrobial agent | |
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 |
5'-methylthioadenosine | 5'-methylthioadenosine: structure 5'-S-methyl-5'-thioadenosine : Adenosine with the hydroxy group at C-5' substituted with a methylthio (methylsulfanyl) group. | thioadenosine | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
stilbamidine | stilbamidine: RN given refers to parent cpd | ||
epz004777 | N-glycosyl compound | ||
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 |
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 | ||
gsk3235025 | GSK3235025: an inhibitor of protein arginine methyltransferase-5 (PRMT5); structure in first source |