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Literature summary for 3.4.21.109 extracted from

  • Desilets, A.; Longpre, J.M.; Beaulieu, M.E.; Leduc, R.
    Inhibition of human matriptase by eglin c variants (2006), FEBS Lett., 580, 2227-2232.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged amino acids 596-855 of matriptase in Escherichia coli strain M15 Homo sapiens
into pQE-vecto and expressed in Escherichia coli M15 strain Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information wild type eglin c has no effect Homo sapiens
R1K'4-eglin different eglin c variants with differing inhibitory potential versus matriptase, construction, expression and purification of eglin c variants and screening for inhibitory potency, overview, R1K'4-eglin has the wild-type Pro45 at P1 position and Tyr49 at P4' position residues replaced with Arg and Lys, respectively, leads to the production of a selective, high affinity and proteolytically stable inhibitor of matriptase, molecular modeling of enzyme-inhibitor complex, overview Homo sapiens
R1K4-eglin wild type eglin c with Pro45 at P1 position and Tyr49 residues at P4 position replaced with Arg and Lys respectively, most potent, selective, high affinity and proteolytically stable inhibitor Homo sapiens
R4R1-eglin with substituted P42 and L45 for arginine residues, variants containing an Arg or Lys at position 49 instead of the original Tyr residue show enhanced inhibition Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information steady-state kinetics Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane matriptase is a type II transmembrane serine protease Homo sapiens 16020
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
29000
-
refolded zymogen Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
by immobilized metal-chelate affinity chromatography and ion exchange chromatography Homo sapiens
recombinant His-tagged amino acids 596-855 of matriptase from Escherichia coli strain M15 by metal affinity chromatography, dialysis, and anion exchange chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
epithelial cancer cell overexpression of the enzyme Homo sapiens
-
epithelium
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
-
?
Boc-Glu-Ala-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Boc-Glu-Ala-Arg + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
More the enzyme belongs ot the type II transmembrane serine protease family Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
9
-
assay at Homo sapiens
9 11 purified enzyme Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000004
-
R1K4-eglin
-
Homo sapiens
0.000004
-
R1K'4-eglin pH 9.0, recombinant His-tagged amino acids 596-855 of matriptase Homo sapiens
0.000026
-
R4R1-eglin
-
Homo sapiens