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protein arginine methyltransferase 5

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Target not currently curated in GtoImmuPdb

Target id: 1256

Nomenclature: protein arginine methyltransferase 5

Abbreviated Name: PRMT5

Family: 2.1.1.- Protein arginine N-methyltransferases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 637 14q11.2 PRMT5 protein arginine methyltransferase 5
Mouse - 637 14 C2 Prmt5 protein arginine N-methyltransferase 5
Rat - - 15p13 Prmt5 protein arginine methyltransferase 5
Previous and Unofficial Names Click here for help
Histone-arginine N-methyltransferase | Jak-binding protein 1 | Jbp1 | HRMT1L5
Database Links Click here for help
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  PRMT5:MEP50 complexed with inhibitor PF-06939999
PDB Id:  7MX7
Ligand:  PF-06939999
Resolution:  2.49Å
Species:  Human
References:  3

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
onametostat Small molecule or natural product Ligand has a PDB structure Hs Inhibition >9.2 pKd 2
pKd >9.2 (Kd <6.28x10-10 M) [2]
Description: Equilibrium dissociation constant determined by surface plasmon resonance spectroscopy, using immobilized Avi-tagged PRMT5:MEP50 protein on streptavidin coated sensors.
EPZ015666 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.3 pKi
pKi 8.3 (Ki 5x10-9 M)
GSK591 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 6
pIC50 8.0 (IC50 1.1x10-8 M) [6]
Description: Measuring inhibition of methylation of histone H4 in an in vitro biochemical assay.
LLY-283 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 2x10-8 M) [4]
Description: Inhibition of methylation of an H4R3 derived peptide substrate in vitro.
DS-437 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 5.2 pIC50 5
pIC50 5.2 (IC50 5.9x10-6 M) [5]
cmp5 [PMID: 25742700] Small molecule or natural product Primary target of this compound Hs Inhibition - - 1
[1]
PF-06939999 Small molecule or natural product Ligand has a PDB structure Hs Inhibition - - 3
[3]

References

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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, 125 (16): 2530-43. [PMID:25742700]

2. Brehmer D, Beke L, Wu T, Millar HJ, Moy C, Sun W, Mannens G, Pande V, Boeckx A, van Heerde E et al.. (2021) Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small Molecule Inhibitor of PRMT5 with Potent Anti-Tumor Activity. Mol Cancer Ther, [Epub ahead of print]. DOI: 10.1158/1535-7163.MCT-21-0367 [PMID:34583982]

3. Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N et al.. (2022) SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance. Mol Cancer Ther, 21 (1): 3-15. [PMID:34737197]

4. 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

5. 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 Lett, 6 (4): 408-12. [PMID:25893041]

6. 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 13/01/2022. Accessed on 28/09/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1256.