protein arginine methyltransferase 6

Target id: 1257

Nomenclature: protein arginine methyltransferase 6

Abbreviated Name: PRMT6

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 6 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 375 1p13.2 PRMT6 protein arginine methyltransferase 6
Mouse - 378 3 48.52 cM Prmt6 protein arginine N-methyltransferase 6
Rat - - 2q41 Prmt6 protein arginine methyltransferase 6
Previous and Unofficial Names
HRMT1L6 | HMT1 hnRNP methyltransferase-like 6
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:  Human HMT1 hnRNP methyltransferase-like protein 6.
PDB Id:  5E8R
Ligand:  MS023
Resolution:  2.55Å
Species:  Human
References:  1

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
MS023 Hs Inhibition 8.2 pKd 2
pKd 8.2 (Kd 6x10-9 M) [2]
MS049 Hs Inhibition 7.1 pKd 5
pKd 7.1 (Kd 8.7x10-8 M) [5]
Description: Isothermal titration calorimetry (ITC) in the presence of SAH
MS023 Hs Inhibition 9.1 pKi 2
pKi 9.1 (Ki 8x10-10 M) [2]
EPZ020411 Hs Inhibition 8.0 pIC50 3
pIC50 8.0 (IC50 1x10-8 M) [3]
MS049 Hs Inhibition 7.4 pIC50 5
pIC50 7.4 (IC50 4.3x10-8 M) [5]
C21 Hs Inhibition 5.1 pIC50 4
pIC50 5.1 (IC50 8.8x10-6 M) [4]

References

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1. Eram MS, Shen Y, Szewczyk MM, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C et al.. (2015) A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem. Biol.,  [Epub ahead of print]. [PMID:26598975]

2. 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.

3. Mitchell LH, Drew AE, Ribich SA, Rioux N, Swinger KK, Jacques SL, Lingaraj T, Boriack-Sjodin PA, Waters NJ, Wigle TJ et al.. (2015) Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound. ACS Med Chem Lett6 (6): 655-9. [PMID:26101569]

4. 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]

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]

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 6. Last modified on 05/04/2017. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1257.