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plasminogen activator, urokinase

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Target not currently curated in GtoImmuPdb

Target id: 2393

Nomenclature: plasminogen activator, urokinase

Family: S1: Chymotrypsin

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 431 10q24 PLAU plasminogen activator, urokinase
Mouse - 433 14 A3 Plau plasminogen activator, urokinase
Rat - 432 15p16 Plau plasminogen activator, urokinase
Previous and Unofficial Names Click here for help
uPA | UPAM | U-plasminogen activator | URK | plasminogen activator
Database Links Click here for help
Specialist databases
MEROPS S01.231 (Hs)
Other databases
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.21.73

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
compound 4 [PMID: 18163548] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
UK-356202 Small molecule or natural product Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 3.7x10-8 M) [1]
WX-UK1 Small molecule or natural product Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 4.1x10-7 M) [3]
upamostat Small molecule or natural product Hs Inhibition - -
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Tissue repair
GO Annotations:  Associated to 1 GO processes
GO:0043403 skeletal muscle tissue regeneration ISO
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Quebec platelet disorder
OMIM: 601709
Orphanet: ORPHA220436

References

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1. Barber CG, Dickinson RP, Fish PV. (2004) Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg. Med. Chem. Lett., 14 (12): 3227-30. [PMID:15149680]

2. Frederickson M, Callaghan O, Chessari G, Congreve M, Cowan SR, Matthews JE, McMenamin R, Smith DM, Vinković M, Wallis NG. (2008) Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. J. Med. Chem., 51 (2): 183-6. [PMID:18163548]

3. Stürzebecher J, Vieweg H, Steinmetzer T, Schweinitz A, Stubbs MT, Renatus M, Wikström P. (1999) 3-Amidinophenylalanine-based inhibitors of urokinase. Bioorg. Med. Chem. Lett., 9 (21): 3147-52. [PMID:10560742]

How to cite this page

S1: Chymotrypsin: plasminogen activator, urokinase. Last modified on 10/03/2014. Accessed on 24/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2393.