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protein arginine methyltransferase 6

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Target id: 1257

Nomenclature: protein arginine methyltransferase 6

Abbreviated Name: PRMT6

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 - 375 1p13.3 PRMT6 protein arginine methyltransferase 6
Mouse - 378 3 F3 Prmt6 protein arginine N-methyltransferase 6
Rat - - 2q41 Prmt6 protein arginine methyltransferase 6
Previous and Unofficial Names Click here for help
HRMT1L6 | HMT1 hnRNP methyltransferase-like 6
Database Links Click here for help
Alphafold Q96LA8 (Hs), Q6NZB1 (Mm)
ChEMBL Target CHEMBL1275221 (Hs)
Ensembl Gene ENSG00000198890 (Hs), ENSMUSG00000049300 (Mm), ENSRNOG00000017187 (Rn)
Entrez Gene 55170 (Hs), 99890 (Mm), 295384 (Rn)
Human Protein Atlas ENSG00000198890 (Hs)
KEGG Gene hsa:55170 (Hs), mmu:99890 (Mm), rno:295384 (Rn)
OMIM 608274 (Hs)
Pharos Q96LA8 (Hs)
SynPHARM 83232 (in complex with MS023)
83231 (in complex with MS023)
UniProtKB Q96LA8 (Hs), Q6NZB1 (Mm)
Wikipedia PRMT6 (Hs)
Selected 3D Structures Click here for help
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
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Protein arginine N-methyltransferase 6 (PRMT6) in complex with SGC6870 inhibitor
PDB Id:  6W6D
Ligand:  SGC6870
Resolution:  1.91Å
Species:  Human
References: 

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 8.2 pKd 2
⤷ pKd 8.2 (Kd 6x10-9 M) [2]
MS049 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.1 pKd 6
⤷ pKd 7.1 (Kd 8.7x10-8 M) [6]
Description: Isothermal titration calorimetry (ITC) in the presence of SAH
MS023 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pKi 2
⤷ pKi 9.1 (Ki 8x10-10 M) [2]
EPZ020411 Small molecule or natural product Primary target of this compound Hs Inhibition 8.0 pIC50 3
⤷ pIC50 8.0 (IC50 1x10-8 M) [3]
MS049 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.4 pIC50 6
⤷ pIC50 7.4 (IC50 4.3x10-8 M) [6]
SGC6870 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.1 pIC50 5
⤷ pIC50 7.1 (IC50 7.7x10-8 M) [5]
C21 Peptide Click here for species-specific activity table Hs Inhibition 5.1 pIC50 4
⤷ pIC50 5.1 (IC50 8.8x10-6 M) [4]
Immuno Process Associations
Immuno Process:  Immune regulation
Immuno Process:  Immune system development

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, Li F, Szewczyk MM, Halabelian L, Chau I, Eram MS, Dela Seña C, Park KS, Meng F, Chen H et al.. (2021) A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6. J Med Chem, 64 (7): 3697-3706. [PMID:33591753]

6. 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 17/02/2021. Accessed on 15/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1257.