Top ▲
Target not currently curated in GtoImmuPdb
Target id: 1252
Nomenclature: protein arginine methyltransferase 1
Abbreviated Name: PRMT1
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 371 | 19q13.33 | PRMT1 | protein arginine methyltransferase 1 | |
Mouse | - | 371 | 7 29.07 cM | Prmt1 | protein arginine N-methyltransferase 1 | |
Rat | - | 353 | 1q22 | Prmt1 | protein arginine methyltransferase 1 |
Previous and Unofficial Names |
ANM1 | HCP1 |
Database Links | |
Alphafold | Q99873 (Hs), Q9JIF0 (Mm), Q63009 (Rn) |
ChEMBL Target | CHEMBL5524 (Hs), CHEMBL1275220 (Rn) |
Ensembl Gene | ENSG00000126457 (Hs), ENSMUSG00000109324 (Mm), ENSRNOG00000026109 (Rn) |
Entrez Gene | 3276 (Hs), 15469 (Mm), 60421 (Rn) |
Human Protein Atlas | ENSG00000126457 (Hs) |
KEGG Gene | hsa:3276 (Hs), mmu:15469 (Mm), rno:60421 (Rn) |
OMIM | 602950 (Hs) |
Pharos | Q99873 (Hs) |
UniProtKB | Q99873 (Hs), Q9JIF0 (Mm), Q63009 (Rn) |
Wikipedia | PRMT1 (Hs) |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
In [3] AMI-1 was only tested against PRMT1, it may therefore be inhibitory of other PRMTs. |
Immuno Process Associations | ||
|
||
|
Physiological Functions | ||||||||
|
||||||||
Physiological Functions Comments | ||||||||
Methylation of histone H4 at Arg3 is associated with increased transcription of various genes via activation of several nuclear receptors such as the estrogen receptor, p53, and NF-κB [1-2]. Specifically, PRMT1 has been demonstrated to methylate the arginine 260 residue of the estrogen receptor α, activating mitogen activated protein kinase (MAPK), protein kinase B (PKB/Akt), and protein kinase C (PKC) mediated signal transduction [5]. |
1. Bedford MT, Clarke SG. (2009) Protein arginine methylation in mammals: who, what, and why. Mol Cell, 33 (1): 1-13. [PMID:19150423]
2. Bedford MT, Richard S. (2005) Arginine methylation an emerging regulator of protein function. Mol Cell, 18 (3): 263-72. [PMID:15866169]
3. Cheng D, Yadav N, King RW, Swanson MS, Weinstein EJ, Bedford MT. (2004) Small molecule regulators of protein arginine methyltransferases. J Biol Chem, 279 (23): 23892-9. [PMID:15056663]
4. Eram MS, Shen Y, Szewczyk MM, Wu H, Senisterra G, Li F, Butler KV, Kaniskan U, Speed BA, dela Sena C et al.. (2015) A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chemical Biology, Just Accepted Manuscript.
5. Le Romancer M, Treilleux I, Leconte N, Robin-Lespinasse Y, Sentis S, Bouchekioua-Bouzaghou K, Goddard S, Gobert-Gosse S, Corbo L. (2008) Regulation of estrogen rapid signaling through arginine methylation by PRMT1. Mol Cell, 31 (2): 212-21. [PMID:18657504]
6. Obianyo O, Causey CP, Jones JE, Thompson PR. (2011) Activity-based protein profiling of protein arginine methyltransferase 1. ACS Chem Biol, 6 (10): 1127-35. [PMID:21838253]
7. Spannhoff A, Machmur R, Heinke R, Trojer P, Bauer I, Brosch G, Schüle R, Hanefeld W, Sippl W, Jung M. (2007) A novel arginine methyltransferase inhibitor with cellular activity. Bioorg Med Chem Lett, 17 (15): 4150-3. [PMID:17570663]
2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 1 . Last modified on 11/12/2015. Accessed on 02/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1252.