protein arginine methyltransferase 1 | 2.1.1.- Protein arginine N-methyltransferases | IUPHAR/BPS Guide to PHARMACOLOGY

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protein arginine methyltransferase 1

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

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 361 19q13 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
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MS023 Hs Inhibition 8.0 pKi 4
pKi 8.0 (Ki 1.1x10-8 M) [4]
C21 Hs Inhibition 5.7 pIC50 6
pIC50 5.7 (IC50 1.8x10-6 M) [6]
AMI-1 Hs Inhibition 5.1 pIC50 3
pIC50 5.1 (IC50 8.81x10-6 M) [3]
RM65 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.
Physiological Functions
Catalyzes the methylation of histone H4 at Arg3 in vivo.
Species:  None
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].


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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 25/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY,