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protein arginine methyltransferase 3

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Target not currently curated in GtoImmuPdb

Target id: 1254

Nomenclature: protein arginine methyltransferase 3

Abbreviated Name: PRMT3

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 - 531 11p15.1 PRMT3 protein arginine methyltransferase 3
Mouse - 532 7 B4 Prmt3 protein arginine N-methyltransferase 3
Rat - 528 1q22 Prmt3 protein arginine methyltransferase 3
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
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Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of protein arginine methyltransferase 3
PDB Id:  3SMQ
Ligand:  compound 1 [PMID: 22795084]
Resolution:  2.3Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Human Protein Arginine Methyltransferase 3 in complex with 1-isoquinolin-6-yl-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl]urea.
PDB Id:  4RYL
Ligand:  SGC707
Resolution:  2.1Å
Species:  Human
References:  2

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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
MS023 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pKi 1
pKi 7.3 (Ki 5.5x10-8 M) [1]
compound 1 [PMID: 22795084] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 5.6 pIC50 3
pIC50 5.6 (IC50 2.5x10-6 M) [3]
Description: IC50 was measured using a SAHH (S-adenosylhomocysteine hydrolase)-coupled in vitro assay.
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SGC707 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Negative 7.3 pKd 2
pKd 7.3 (Kd 5.3x10-8 M) [2]
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0031397 negative regulation of protein ubiquitination IDA

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. Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I et al.. (2015) A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl, 54 (17): 5166-70. [PMID:25728001]

3. Siarheyeva A, Senisterra G, Allali-Hassani A, Dong A, Dobrovetsky E, Wasney GA, Chau I, Marcellus R, Hajian T, Liu F et al.. (2012) An allosteric inhibitor of protein arginine methyltransferase 3. Structure, 20 (8): 1425-35. [PMID:22795084]

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 3. Last modified on 11/12/2015. Accessed on 18/06/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1254.