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Literature summary for 3.4.24.24 extracted from

  • Cheng, D.; Shen, Q.; Nan, F.; Qian, Z.; Ye, Q.Z.
    Purification and characterization of catalytic domains of gelatinase A with or without fibronectin insert for high-throughput inhibitor screening (2003), Protein Expr. Purif., 27, 63-74.
    View publication on PubMed

Application

Application Comment Organism
medicine attractive therapeutic target for cancer invasion and metastasis, morbidity and mortality of cancer patients are directly related to the ability of tumor cells to metastasize, gelatinase A is required by metastazing tumor cells to traverse basement membrane at tissue bounaries and in blood vessels, therefore this enzyme is a promising target for the development of antitumor drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
cloned and overexpressed in a bacterial system, Escherichia coli BL21(DE3)pLysS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,10-phenanthroline
-
Homo sapiens
4-Aminobenzoyl-Gly-Pro-D-Leu-D-Ala-NHOH
-
Homo sapiens
benzyloxycarbonyl-L-Trp-OH
-
Homo sapiens
EDTA
-
Homo sapiens
galardin
-
Homo sapiens
ter-butyloxycarbonyl-L-Trp-OH
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0057
-
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens
0.0099
-
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
0.059
-
Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Ala-Lys(N-Me-Abz)-NH2 pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
0.118
-
Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Ala-Lys(N-Me-Abz)-NH2 pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens
0.136
-
Ac-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-OEt pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
0.172
-
Ac-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-OEt pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ active site requires calcium ions Homo sapiens
Zn2+ active site requires zinc ions Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
20000
-
GaCD, without fibronectin-like insert, SDS-PAGE Homo sapiens
38000
-
GaCDfn, with fibronectin-like insert, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
human
-

Purification (Commentary)

Purification (Comment) Organism
with or without fibronectin-like insert Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.368
-
GaCDfn, with fibronectin-like insert Homo sapiens
11.8
-
GaCD, without fibronectin-like insert Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-OEt + H2O
-
Homo sapiens ?
-
?
Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Ala-Lys(N-Me-Abz)-NH2 + H2O
-
Homo sapiens ?
-
?
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 + H2O
-
Homo sapiens ?
-
?
additional information Mca-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 and DABCYL-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Arg-EDANS are no substrates Homo sapiens ?
-
?
Type IV collagen + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
gelatinase A
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.6
-
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens
1.7
-
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
4.7
-
Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Ala-Lys(N-Me-Abz)-NH2 pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens
5.4
-
Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Ala-Lys(N-Me-Abz)-NH2 pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
16.7
-
Ac-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-OEt pH 7.5, 37°C, GaCD, without fibronectin-like insert Homo sapiens
19.5
-
Ac-Pro-Leu-Gly-[2-mercapto-4-methylpentanoyl]-Leu-Gly-OEt pH 7.5, 37°C, GaCDfn, with fibronectin-like insert Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
-
Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
5 10
-
Homo sapiens