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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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 431 10q22.2 PLAU plasminogen activator, urokinase
Mouse - 433 14 11.53 cM 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
Alphafold P00749 (Hs), P06869 (Mm), P29598 (Rn)
BRENDA 3.4.21.73
ChEMBL Target CHEMBL3286 (Hs), CHEMBL1075311 (Mm), CHEMBL1075245 (Rn)
DrugBank Target P00749 (Hs)
Ensembl Gene ENSG00000122861 (Hs), ENSMUSG00000021822 (Mm), ENSRNOG00000010516 (Rn)
Entrez Gene 5328 (Hs), 18792 (Mm), 25619 (Rn)
Human Protein Atlas ENSG00000122861 (Hs)
KEGG Enzyme 3.4.21.73
KEGG Gene hsa:5328 (Hs), mmu:18792 (Mm), rno:25619 (Rn)
OMIM 191840 (Hs)
Orphanet ORPHA223447 (Hs)
Pharos P00749 (Hs)
RefSeq Nucleotide NM_002658 (Hs), NM_001145031 (Hs), NM_008873 (Mm), NM_013085 (Rn)
RefSeq Protein NP_002649 (Hs), NP_001138503 (Hs), NP_032899 (Mm), NP_037217 (Rn)
SynPHARM 78434 (in complex with compound 4 [PMID: 18163548])
UniProtKB P00749 (Hs), P06869 (Mm), P29598 (Rn)
Wikipedia PLAU (Hs)
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
BB2-50F Small molecule or natural product Ligand has a PDB structure Hs Inhibition 6.7 pKi 2
⤷ pKi 6.7 (Ki 1.83x10-7 M) [2]
WX-UK1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pKi 4
⤷ pKi 6.2 (Ki 6.5x10-7 M) [4]
compound 4 [PMID: 18163548] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.7 pIC50 3
⤷ pIC50 7.7 (IC50 2x10-8 M) [3]
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 Click here for species-specific activity table Hs Inhibition 6.4 pIC50 5
⤷ pIC50 6.4 (IC50 4.1x10-7 M) [5]
upamostat Small molecule or natural product Hs Inhibition - -
⤷
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Immuno Process:  Tissue repair
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. Buckley BJ, Aboelela A, Minaei E, Jiang LX, Xu Z, Ali U, Fildes K, Cheung CY, Cook SM, Johnson DC et al.. (2018) 6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer. J Med Chem, 61 (18): 8299-8320. [PMID:30130401]

3. 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]

4. Setyono-Han B, Stürzebecher J, Schmalix WA, Muehlenweg B, Sieuwerts AM, Timmermans M, Magdolen V, Schmitt M, Klijn JG, Foekens JA. (2005) Suppression of rat breast cancer metastasis and reduction of primary tumour growth by the small synthetic urokinase inhibitor WX-UK1. Thromb Haemost, 93 (4): 779-86. [PMID:15841327]

5. 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 05/02/2024. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2393.