Target type: molecularfunction
Catalysis of the addition of a methyl group to either of the unmethylated terminal nitrogen atoms (also called omega nitrogen) in peptidyl-arginine to form an omega-N-G-monomethylated arginine residue. The reaction is S-adenosyl-L-methionine + [protein]-L-arginine = S-adenosyl-L-homocysteine + [protein]-Nomega-methyl-L-arginine. [EC:2.1.1.321, PMID:14705965, RESID:AA0069]
Protein-arginine omega-N monomethyltransferase activity is a catalytic activity that involves the transfer of a methyl group from a donor molecule, typically S-adenosyl methionine (SAM), to the omega-N position of an arginine residue within a protein substrate. This methylation event can significantly alter the structure and function of the target protein. The precise molecular function of this activity depends on the specific protein substrate and the cellular context.
Here are some key aspects of protein-arginine omega-N monomethyltransferase activity:
1. Substrate Specificity: These enzymes exhibit varying degrees of substrate specificity, targeting specific arginine residues within particular protein substrates. This specificity is often determined by the surrounding amino acid sequence and the overall conformation of the target protein.
2. Methylation Site: The methylation occurs at the omega-N position of the arginine residue, which is the terminal nitrogen atom of the guanidinium group. This modification introduces a small, positively charged methyl group.
3. Impact on Protein Function: Methylation can significantly impact protein function in various ways, including:
- Altering protein-protein interactions by modulating electrostatic interactions or creating new binding sites.
- Changing protein stability and folding dynamics.
- Modifying enzyme activity by affecting substrate binding or catalytic efficiency.
- Regulating protein localization and trafficking within the cell.
4. Cellular Roles: Protein-arginine omega-N monomethyltransferases are involved in diverse cellular processes, including:
- Signal transduction pathways: Modifying signaling proteins to regulate downstream responses.
- Gene expression: Regulating the activity of transcription factors and chromatin remodeling complexes.
- Cellular metabolism: Modulating the activity of enzymes involved in metabolic pathways.
- Development and differentiation: Controlling cell fate decisions and tissue morphogenesis.
5. Disease Relevance: Dysregulation of protein-arginine omega-N monomethyltransferases has been implicated in various diseases, including cancer, neurodevelopmental disorders, and autoimmune diseases.
Overall, protein-arginine omega-N monomethyltransferase activity plays a critical role in regulating a wide range of cellular processes by modifying the structure and function of target proteins. Understanding the molecular details of this activity is essential for developing targeted therapies for various diseases.'
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Protein | Definition | Taxonomy |
---|---|---|
Protein arginine N-methyltransferase 7 | A protein arginine N-methyltransferase 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NVM4] | Homo sapiens (human) |
Protein arginine N-methyltransferase 1 | A protein arginine N-methyltransferase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99873] | 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) |
Protein arginine N-methyltransferase 3 | A protein arginine N-methyltransferase 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60678] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
fluorescite | fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | benzoic acids; cyclic ketone; hydroxy monocarboxylic acid; organic heterotricyclic compound; phenols; xanthene dye | fluorescent dye; radioopaque medium |
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 |
saccharin | saccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent. Saccharin: Flavoring agent and non-nutritive sweetener. | 1,2-benzisothiazole; N-sulfonylcarboxamide | environmental contaminant; sweetening agent; 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 |
suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
alizarin | dihydroxyanthraquinone | chromophore; dye; plant metabolite | |
7-amino-4-hydroxy-2-naphthalenesulfonic acid | 7-amino-4-hydroxy-2-naphthalenesulfonic acid : An aminonaphthalenesulfonic acid that is 2-naphthalenesulfonic acid substituted by an amino group at position 7 and a hydroxy group at position 4 respectively. 7-amino-4-hydroxy-2-naphthalenesulfonic acid: structure given in first source | aminonaphthalenesulfonic acid; naphthols | metabolite |
1-naphthol-8-amino-3,6-disulfonic acid | 1-naphthol-8-amino-3,6-disulfonic acid: dye and found in industrial waste | ||
methyl red | methyl red : An azo dye consisting of benzoic acid substituted at position 2 by a 4-[(dimethylamino)phenyl]diazenyl group. methyl red: RN given refers to parent cpd; structure | ||
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 | |
fluorone black | fluorone Black: structure | ||
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 | ||
mbx 1090 | |||
unc 0321 | 7-(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 source | quinazolines | |
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 | ||
sgc707 |