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
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 M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C et al.. (2016) A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem. Biol., 11 (3): 772-781. [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 Lett, 6 (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 21/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1257.