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Literature summary for 3.4.21.73 extracted from

  • Lin, Z.; Jiang, L.; Yuan, C.; Jensen, J.K.; Zhang, X.; Luo, Z.; Furie, B.C.; Furie, B.; Andreasen, P.A.; Huang, M.
    Structural basis for recognition of urokinase-type plasminogen activator by plasminogen activator inhibitor-1 (2011), J. Biol. Chem., 286, 7027-7032.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression of mutant S195A in Pichia pastoris strain X-33 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
PAI-1/uPA mutant S195A in a Michaelis complex, hanging drop method, 20°C, mixing of equal volumes of protein solution, containing 10 mg/ml protein in 20 mM Tris-HCl, pH 8.0, and 150 mM NaCl, and precipitant solution, containing 1.4 M ammonium sulfate and 0.1 M Tris-HCl, pH 7.4, 4 months, the cryoprotectant solution contains 30% glycerol, 1.6 M ammonium sulfate, and 0.1 M Tris-HCl, pH 7.4, X-ray diffraction structure determination and analysis at 2.3 A resolution, molecular replacement Homo sapiens

Protein Variants

Protein Variants Comment Organism
S195A site-directed mutagenesis, the mutant contains the catalytically inactive form of the human uPA protease domain Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
plasminogen activator inhibitor-1 PAI-1, specifically and rapidly inhibits urokinase-type plasminogen activator uPA and tissue-type plasminogen activator, tPA, EC 3.4.21.68. The PAI-1 reactive center loop serves as a bait to attract uPA onto the top of the PAI-1 molecule. P4–P3' residues of the reactive center loop interact extensively with the uPA catalytic site, accounting for about two-thirds of the total contact area, also almost all uPA exosite loops, including the 37-, 60-, 97-, 147-, and 217-loops, are involved in the interaction with PAI-1, of the residues of the 37-loop, Arg-E37a plays the most important role, Michaelis complex formation, overview. The recombinant stable His-tagged PAI-1 mutant 14-1B containing four point mutations N150H, K154T, Q319L, and M354I, is expressed in Escherichia coli strain C41(DE3) using the expression vector pT7-PL Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00749
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-

Purification (Commentary)

Purification (Comment) Organism
recombinant mutant S195A from Pichia pastoris strain X-33 by nickel affinity chromatography and gel filtration Homo sapiens

Synonyms

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

General Information

General Information Comment Organism
physiological function plasminogen activator, together with urokinase-type plasminogen activator inhibitor-1, PAI-1, plays a pivotal role in fibrinolysis, cell migration, and tissue remodeling Homo sapiens