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coactivator associated arginine methyltransferase 1

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Target not currently curated in GtoImmuPdb

Target id: 1255

Nomenclature: coactivator associated arginine methyltransferase 1

Abbreviated Name: PRMT4

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 - 608 19p13.2 CARM1 coactivator associated arginine methyltransferase 1
Mouse - 608 9 A3 Carm1 coactivator-associated arginine methyltransferase 1
Rat - 651 8q13 Carm1 coactivator-associated arginine methyltransferase 1
Previous and Unofficial Names Click here for help
Histone-arginine methyltransferase CARM1 | protein arginine N-methyltransferase 4
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Coactivator-associated arginine methyltransferase 1 (PRMT4) crystalised with inhibitor TP-064.
PDB Id:  5U4X
Ligand:  TP-064
Resolution:  1.88Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.1.1.125

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
MS049 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.0 pKd 5
pKd 7.0 (Kd 1x10-7 M) [5]
Description: Isothermal titration calorimetry (ITC) in the presence of SAH
MS023 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pKi 1
pKi 7.6 (Ki 2.3x10-8 M) [1]
BIIB021 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >8.0 pIC50 4
pIC50 >8.0 (IC50 <1x10-8 M) [4]
Description: In vitro methylation of H3 (1-25).
MS049 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 5
pIC50 7.5 (IC50 3.4x10-8 M) [5]
BMS pyrazole inhibitor 7f Small molecule or natural product Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
SGC2085 Small molecule or natural product Primary target of this compound Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5x10-8 M) [2]
compound 17f [PMID: 19632837] Small molecule or natural product Hs Inhibition 7.2 pIC50 6
pIC50 7.2 (IC50 7x10-8 M) [6]
Inhibitor Comments
BMS pyrazole inhibitor 7f appears to be selective for PRMT4 (CARM1) across a panel of tested proteins [3].

References

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1. 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.

2. Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M et al.. (2016) Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J. Med. Chem., 59 (14): 6838-47. [PMID:27390919]

3. Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A et al.. (2009) Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1). Bioorg. Med. Chem. Lett., 19 (11): 2924-7. [PMID:19419866]

4. SGC. TP-064 A Chemical Probe For PRMT4. Accessed on 05/04/2017. Modified on 05/04/2017. thesgc.org, http://www.thesgc.org/chemical-probes/TP-064

5. Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, Ferreira de Freitas R, Senisterra G, Li F, Schapira M, Brown PJ et al.. (2016) Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J. Med. Chem., 59 (19): 9124-9139. [PMID:27584694]

6. Wan H, Huynh T, Pang S, Geng J, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L et al.. (2009) Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies. Bioorg. Med. Chem. Lett., 19 (17): 5063-6. [PMID:19632837]

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: coactivator associated arginine methyltransferase 1. Last modified on 05/04/2017. Accessed on 02/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1255.