protein arginine methyltransferase 5

Target id: 1256

Nomenclature: protein arginine methyltransferase 5

Abbreviated Name: PRMT5

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 5 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 636 14q11.2 PRMT5 protein arginine methyltransferase 5
Mouse - 636 14 27.82 cM Prmt5 protein arginine N-methyltransferase 5
Rat - - 15p13 Prmt5 protein arginine methyltransferase 5
Previous and Unofficial Names
Histone-arginine N-methyltransferase | Jak-binding protein 1 | Jbp1 | HRMT1L5
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
SynPHARM
UniProtKB
Wikipedia

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
EPZ015666 Hs Inhibition 8.3 pKi
pKi 8.3 (Ki 5x10-9 M)
GSK591 Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1.1x10-8 M) [4]
Description: Measuring inhibition of methylation of histone H4 in an in vitro biochemical assay.
LLY-283 Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
Description: Inhibition of methylation of an H4R3 derived peptide substrate in vitro.
DS-437 Hs Inhibition 5.2 pIC50 3
pIC50 5.2 (IC50 5.9x10-6 M) [3]
cmp5 [PMID: 25742700] Hs Inhibition - - 1
[1]

References

Show »

1. Alinari L, Mahasenan KV, Yan F, Karkhanis V, Chung JH, Smith EM, Quinion C, Smith PL, Kim L, Patton JT et al.. (2015) Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation. Blood,  [Epub ahead of print]. [PMID:25742700]

2. SGC. LLY-283 A Chemical Probe For PRMT5. Accessed on 05/04/2017. Modified on 05/04/2017. thesgc.org, http://www.thesgc.org/chemical-probes/LLY-283

3. Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. (2015) Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett6 (4): 408-12. [PMID:25893041]

4. Structural Genomics Consortium. GSK591 A chemical probe for PRMT5. Accessed on 11/12/2015. Modified on 11/12/2015. The Structural Genomics Consortium, http://www.thesgc.org/chemical-probes/GSK591

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 5 . Last modified on 05/04/2017. Accessed on 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1256.