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Literature summary for 3.4.21.73 extracted from

  • Botkjaer, K.A.; Fogh, S.; Bekes, E.C.; Chen, Z.; Blouse, G.E.; Jensen, J.M.; Mortensen, K.K.; Huang, M.; Deryugina, E.; Quigley, J.P.; Declerck, P.J.; Andreasen, P.A.
    Targeting the autolysis loop of urokinase-type plasminogen activator with conformation-specific monoclonal antibodies (2011), Biochem. J., 438, 39-51.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.73

Inhibitors

Inhibitors Comment Organism Structure
additional information the autolysis loop in the catalytic domain of uPA is a potential inhibitory target. Three antibodies are potent inhibitors of uPA activity, two pro-uPA-specific ones by inhibiting conversion of pro-uPA to active uPA and an active uPA-specific antibody by shielding the access of plasminogen to the active site, overview. The conformation-specific antibodies mAb-112 and mAb-12E6B10 are useful to selectively stain pro-uPA or active uPA on the surface of cultured cells. Antibody mAb-112 is a non-competitive inhibitor of S-2444 cleavage by uPA with a Ki similar to the Kd for mAb-112 binding to active two-chain uPA. The epitopes of the conformation-specific antibodies are all localized to the activation and/or autolysis loop, binding kinetic analysis and models of the three-dimensional structures, overview Homo sapiens
plasminogen activator inhibitor PAI-1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification the zymogen form pro-uPA is cleaved to the active two-chain uPA Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation pro-uPA and mature uPA Homo sapiens
-
U-937 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Glu-Gly-Arg-4-nitroanilide + H2O a uPA substrate S-2444 Homo sapiens D-Glu-Gly-Arg + 4-nitroaniline
-
 ?

Subunits

Subunits Comment Organism
More models of the three-dimensional structures of uPA and pro-uPA, and homology model of the catalytic domain of pro-uPA, overview Homo sapiens

Synonyms

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

General Information

General Information Comment Organism
additional information there exists a direct link between conformational changes of the autolysis loop and the creation of a catalytically mature active site. The conformation-specific antibodies mAb-112 and mAb-12E6B10 are useful to selectively stain pro-uPA or active uPA on the surface of cultured cells Homo sapiens