protein arginine methyltransferase 3

Target id: 1254

Nomenclature: protein arginine methyltransferase 3

Abbreviated Name: PRMT3

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

   GtoImmuPdb view: OFF :     Currently no data for protein arginine methyltransferase 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 531 11p15.1 PRMT3 protein arginine methyltransferase 3
Mouse - 532 7 31.44 cM Prmt3 protein arginine N-methyltransferase 3
Rat - 528 1q22 Prmt3 protein arginine methyltransferase 3
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
MS023 Hs Inhibition 7.3 pKi 1
pKi 7.3 (Ki 5.5x10-8 M) [1]
compound 1 [PMID: 22795084] 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 Affinity Units Reference
SGC707 Hs Negative 7.3 pKd 2
pKd 7.3 (Kd 5.3x10-8 M) [2]

References

Show »

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. Structure20 (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 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1254.