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Literature summary for 3.4.21.73 extracted from

  • Liu, Z.; Kromann-Hansen, T.; Lund, I.K.; Hosseini, M.; Jensen, K.J.; Hoeyer-Hansen, G.; Andreasen, P.A.; Soerensen, H.P.
    Interconversion of active and inactive conformations of urokinase-type plasminogen activator (2012), Biochemistry, 51, 7804-7811.
    View publication on PubMed
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Protein Variants

Protein Variants Comment Organism
E137A site-directed mutagenesis, introduction of the mutations F40Y or E137A into muPA(16-243) increased exposure of the N-terminus (Ile16) and resulted in large changes in the thermodynamic parameters for mupain-1-16 binding Mus musculus
F40Y site-directed mutagenesis, introduction of the mutations F40Y or E137A into muPA(16-243) increased exposure of the N-terminus (Ile16) and resulted in large changes in the thermodynamic parameters for mupain-1-16 binding Mus musculus
additional information the distorted state of truncated mutant muPA(16-243) is conformationally ordered upon binding of ligands to the active site and upon binding of mU3 to the 37- and 70-loop Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
antibody mU3 binding of mU3 to the 37- and 70-loops, the antibody stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mU3 Mus musculus
mupain-1-16 the inhibitor stabilizes the active conformation of the enzyme, the N-terminus (Ile16) of the truncated enzyme muPA(16-243) is less exposed upon binding of mupain-1-16 Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
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-
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Synonyms

Synonyms Comment Organism
uPA
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 Mus musculus
Urokinase-type plasminogen activator
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 Mus musculus

General Information

General Information Comment Organism
additional information the catalytic activity of serine proteases depends on a salt-bridge between the amino group of residue 16 and the side chain of Asp194. The salt-bridge stabilizes the oxyanion hole and the S1 specificity pocket of the protease. Some serine proteases exist in only partially active forms, in which the amino group of residue 16 is exposed to the solvent. Such a partially active state is assumed by a truncated form of the murine urokinase-type plasminogen activator consisting of residues 16-243, allosteric interconversion analysis between partially active states and the fully active state, overview. Both a monoclonal antibody (mU3) and a peptidic inhibitor (mupain-1-16) stabilize the active state Mus musculus