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plasminogen

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Target not currently curated in GtoImmuPdb

Target id: 2394

Nomenclature: plasminogen

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 810 6q26 PLG plasminogen
Mouse - 812 17 8.5 cM Plg plasminogen
Rat - 812 1q11 Plg plasminogen
Previous and Unofficial Names Click here for help
angiostatin | Pg
Database Links Click here for help
Specialist databases
MEROPS S01.233 (Hs)
Other databases
Alphafold P00747 (Hs), P20918 (Mm), Q01177 (Rn)
BRENDA 3.4.21.7
ChEMBL Target CHEMBL1801 (Hs), CHEMBL1075299 (Mm), CHEMBL3204 (Rn)
DrugBank Target P00747 (Hs)
Ensembl Gene ENSG00000122194 (Hs), ENSMUSG00000059481 (Mm), ENSRNOG00000017223 (Rn)
Entrez Gene 5340 (Hs), 18815 (Mm), 85253 (Rn)
Human Protein Atlas ENSG00000122194 (Hs)
KEGG Enzyme 3.4.21.7
KEGG Gene hsa:5340 (Hs), mmu:18815 (Mm), rno:85253 (Rn)
OMIM 173350 (Hs)
Orphanet ORPHA117886 (Hs)
Pharos P00747 (Hs)
RefSeq Nucleotide NM_000301 (Hs), NM_008877 (Mm), NM_053491 (Rn)
RefSeq Protein NP_000292 (Hs), NP_032903 (Mm), NP_445943 (Rn)
SynPHARM 78429 (in complex with 6-aminocaproic acid)
78427 (in complex with tranexamic acid)
UniProtKB P00747 (Hs), P20918 (Mm), Q01177 (Rn)
Wikipedia PLG (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.7

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
bis-triazole derivative 10 Small molecule or natural product Hs Inhibition 9.1 pKi 2
⤷ pKi 9.1 (Ki 7.7x10-10 M) [2]
WX-UK1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pKi 3
⤷ pKi 5.8 (Ki 1.46x10-6 M) [3]
aprotinin {Sp: Bovine} Peptide Approved drug Primary target of this compound Hs Binding 6.8 pIC50 4
⤷ pIC50 6.8 (IC50 1.6x10-7 M) [4]
6-aminocaproic acid Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Binding 4.4 pIC50 1
⤷ pIC50 4.4 (IC50 4x10-5 M) [1]
Description: Measuring inhibition of fibrinolysis in plasma.
tranexamic acid Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Binding 3.6 pIC50 4
⤷ pIC50 3.6 (IC50 2.41x10-4 M) [4]
Immuno Process Associations
Immuno Process:  Chemotaxis & migration
Immuno Process:  Inflammation
Immuno Process:  Tissue repair
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Hypoplasminogenemia
Synonyms: Plasminogen deficiency type 1
OMIM: 217090
Orphanet: ORPHA722
Disease:  Ligneous conjunctivitis
OMIM: 217090
Orphanet: ORPHA97231

References

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1. Cheng L, Pettersen D, Ohlsson B, Schell P, Karle M, Evertsson E, Pahlen S, Jonforsen M, Plowright AT, Bostrom J et al.. (2014) Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. ACS Med Chem Lett, 5 (5): 538-543. [PMID:24900876]

2. Saupe SM, Steinmetzer T. (2012) A new strategy for the development of highly potent and selective plasmin inhibitors. J Med Chem, 55 (3): 1171-80. [PMID:22276953]

3. 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]

4. Sperzel M, Huetter J. (2007) Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost, 5 (10): 2113-8. [PMID:17666018]

How to cite this page

S1: Chymotrypsin: plasminogen. Last modified on 17/05/2022. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2394.