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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

Contents:

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
Alphafold O60678 (Hs), Q922H1 (Mm), O70467 (Rn)
ChEMBL Target CHEMBL5891 (Hs)
Ensembl Gene ENSG00000185238 (Hs), ENSMUSG00000030505 (Mm), ENSRNOG00000014829 (Rn)
Entrez Gene 10196 (Hs), 71974 (Mm), 89820 (Rn)
Human Protein Atlas ENSG00000185238 (Hs)
KEGG Gene hsa:10196 (Hs), mmu:71974 (Mm), rno:89820 (Rn)
OMIM 603190 (Hs)
Pharos O60678 (Hs)
SynPHARM 79359 (in complex with compound 1 [PMID: 22795084])
82339 (in complex with SGC707)
UniProtKB O60678 (Hs), Q922H1 (Mm), O70467 (Rn)
Wikipedia PRMT3 (Hs)
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

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 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

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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1254.