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Literature summary for 3.4.21.73 extracted from

  • Skeldal, S.; Larsen, J.V.; Pedersen, K.E.; Petersen, H.H.; Egelund, R.; Christensen, A.; Jensen, J.K.; Gliemann, J.; Andreasen, P.A.
    Binding areas of urokinase-type plasminogen activator-plasminogen activator inhibitor-1 complex for endocytosis receptors of the low-density lipoprotein receptor family, determined by site-directed mutagenesis (2006), FEBS J., 273, 5143-5159.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant enzymes in HEK-293T cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information deletion of the N-terminal growth factor domain of uPA reduced the affinity for enzyme receptors 2-4fold, depending on the receptor, e.g. VLDLR-I, SorLA, or LRP-1A, and deletion of both the growth factor domain and the kringle reduced the receptor affinity 7fold, overview Homo sapiens
R178A/R179A/R181A site-directed mutagenesis, the mutant shows reduced receptor binding Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
plasminogen activator inhibitor-1 i.e. PAI-1, complexes the enzyme, binding structure, the 10-100-fold higher affinity of the uPA-PAI-1 complex compared with the free components depends on the bonus effect of bringing the binding areas on uPA and PAI-1 together on the same binding entity, overview, inhibitor mutants K71A/R78A/Y81A/K82A, K82A-R120A, and R78A-K124A show reduced binding to the enzyme and the enzyme receptors, effects of several mutations of the inhibitor protein on complex formation and endocytosis, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information binding kinetics of enzyme with enzyme receptors VLDLR-I, SorLA, or LRP-1A , overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme-plasminogen activator inhibitor-1 complex in intenalized by endocytosis via binding of membrane-bound receptors, overview ?
-
?
plasminogen + H2O Homo sapiens
-
plasmin + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme-plasminogen activator inhibitor-1 complex in intenalized by endocytosis via binding of membrane-bound receptors, overview Homo sapiens ?
-
?
plasminogen + H2O
-
Homo sapiens plasmin + ?
-
?
S-2444 + H2O i.e. pyro-Glu-Gly-Arg-p-nitroanilide, a chromogenic substrate Homo sapiens pyroGlu-Gly-Arg + 4-nitroaniline
-
?

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens