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protein arginine methyltransferase 1

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Target not currently curated in GtoImmuPdb

Target id: 1252

Nomenclature: protein arginine methyltransferase 1

Abbreviated Name: PRMT1

Family: 2.1.1.- Protein arginine N-methyltransferases

Gene and Protein Information Click here for help
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 Click here for help
ANM1 | HCP1
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MS023 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pKi 4
pKi 8.0 (Ki 1.1x10-8 M) [4]
C21 Peptide Click here for species-specific activity table Hs Inhibition 5.7 pIC50 6
pIC50 5.7 (IC50 1.8x10-6 M) [6]
AMI-1 Small molecule or natural product Hs Inhibition 5.1 pIC50 3
pIC50 5.1 (IC50 8.81x10-6 M) [3]
RM65 Small molecule or natural product Hs Inhibition 4.3 pIC50 7
pIC50 4.3 (IC50 5.54x10-5 M) [7]
Inhibitor Comments
In [3] AMI-1 was only tested against PRMT1, it may therefore be inhibitory of other PRMTs.
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0045648 positive regulation of erythrocyte differentiation IMP
GO:0045652 regulation of megakaryocyte differentiation IDA
GO:0045653 negative regulation of megakaryocyte differentiation IDA
Immuno Process:  Immune system development
GO Annotations:  Associated to 3 GO processes
GO:0045648 positive regulation of erythrocyte differentiation IMP
GO:0045652 regulation of megakaryocyte differentiation IDA
GO:0045653 negative regulation of megakaryocyte differentiation IDA
Physiological Functions Click here for help
Catalyzes the methylation of histone H4 at Arg3 in vivo.
Species:  None
Tissue: 
References:  1-2
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].

References

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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]

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 1 . Last modified on 11/12/2015. Accessed on 08/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1252.