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Literature summary for 3.4.21.73 extracted from

  • Massey, A.P.; Harley, W.R.; Pasupuleti, N.; Gorin, F.A.; Nantz, M.H.
    2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator (2012), Bioorg. Med. Chem. Lett., 22, 2635-2639.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide i.e. amiloride, selectively inhibits the enzyme, but not tissue plasminogen activator or other serine protease members of the trypsin superfamily Homo sapiens
additional information 2-amidino analogues of glycine-amiloride conjugates as inhibitors of urokinase-type plasminogen activator, design and synthesis, overview. Substitution of C2-acylguanidine of C5-glycyl-amiloride with amidine and amidoxime groups, respectively. Importance of maintaining C5-hydrophobicity Homo sapiens
PAI-1
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
plasminogen + H2O Homo sapiens
-
 plasmin + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P00749
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification the enzyme is synthesized intracellularly as a single chain, inactive proenzyme, is secreted, binds to its receptor and is activated more than 30fold Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
plasminogen + H2O
-
 Homo sapiens plasmin + ?
-
 ?

Synonyms

Synonyms Comment Organism
uPA
-
 Homo sapiens
Urokinase-type plasminogen activator
-
 Homo sapiens

General Information

General Information Comment Organism
evolution the enzyme belongs to the trypsin superfamily of enzymes Homo sapiens
metabolism the urokinase plasminogen activation pathways are comprised of urokinase-type plasminogen activator, its plasmalemmal receptor, and extracellular plasminogen Homo sapiens
additional information highly invasive cancers of breast, brain, prostate and lung notably have increased levels of the enzyme, its receptor uPAR, or an endogenous inhibitor protein PAI-1, which correlate with the propensity of a cancer cell type to invade and to disseminate Homo sapiens
physiological function activated extracellular enzyme cleaves plasminogen to plasmin, which initiates an extracellular protease cascade to degrade the extracellular matrix and facilitate cellular processes such as cellular migration, angiogenesis, tissue remodeling, and wound repair Homo sapiens