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Literature summary for 3.4.22.1 extracted from

  • Sosic, I.; Mitrovic, A.; Curic, H.; Knez, D.; Brodnik Zugelj, H.; Stefane, B.; Kos, J.; Gobec, S.
    Cathepsin B inhibitors Further exploration of the nitroxoline core (2018), Bioorg. Med. Chem. Lett., 28, 1239-1247 .
    View publication on PubMed
Search for more literature for 3.4.22.1

Inhibitors

Inhibitors Comment Organism Structure
1,1'-[[3-(5-nitroquinolin-8-yl)furan-2,5-diyl]dibenzene-4,1-diyl]diethanone
-
 Homo sapiens
1-[4-[3-(5-nitroquinolin-8-yl)furan-2-yl]phenyl]ethan-1-one
-
 Homo sapiens
2-methyl-5-nitroquinolin-8-ol
-
 Homo sapiens
4-methoxy-3-(3-methoxypropoxy)-1-(5-nitroquinolin-8-yl)pyridin-1-ium
-
 Homo sapiens
8-hydroxy-5-nitroquinoline-2-carbonitrile
-
 Homo sapiens
N-(1-cyanocyclopropyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
 Homo sapiens
N-(cyanomethyl)-5-nitroquinoline-8-carboxamide
-
 Homo sapiens
N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide
-
 Homo sapiens
N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
 Homo sapiens
N-benzyl-N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide
-
 Homo sapiens
N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-2-carboxamide
-
 Homo sapiens
N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide
-
 Homo sapiens
N-[[1-(1,3-benzothiazol-2-yl)piperidin-3-yl]methyl]-8-hydroxy-5-nitroquinoline-7-carboxamide
-
 Homo sapiens
N-[[1-(1,3-benzoxazol-2-yl)piperidin-3-yl]methyl]-8-hydroxy-5-nitroquinoline-7-carboxamide
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P07858
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH + H2O exopeptidase activity Homo sapiens ?
-
 ?
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin + H2O endopeptidase activity Homo sapiens benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.035
-
 N-benzyl-N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.118
-
 4-methoxy-3-(3-methoxypropoxy)-1-(5-nitroquinolin-8-yl)pyridin-1-ium substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.128
-
 N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.142
-
 8-hydroxy-5-nitroquinoline-2-carbonitrile substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.156
-
 N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-2-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.16
-
 N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.181
-
 2-methyl-5-nitroquinolin-8-ol substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.182
-
 N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.185
-
 N-benzyl-N-(cyanomethyl)-8-hydroxy-5-nitroquinoline-7-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.185
-
 N-(1-cyanocyclopropyl)-8-hydroxy-5-nitroquinoline-7-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.19
-
 N-(cyanomethyl)-5-nitroquinoline-8-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.201
-
 N-(cyanomethyl)-8-hydroxy-5,7-dinitroquinoline-2-carboxamide substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.214
-
 8-hydroxy-5-nitroquinoline-2-carbonitrile substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.24
-
 N-(cyanomethyl)-5-nitroquinoline-8-carboxamide substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.323
-
 4-methoxy-3-(3-methoxypropoxy)-1-(5-nitroquinolin-8-yl)pyridin-1-ium substrate: benzyloxycarbonyl-Arg-Arg-AMC, endopeptidase activity, pH and temperature not specified in the publication Homo sapiens
0.469
-
 2-methyl-5-nitroquinolin-8-ol substrate: 2-aminobenzoy-Gly-Ile-Val-Arg-Ala-Lys(Dnp)-OH, exopeptidase activity, pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
physiological function the enzyme is involved in intracellular proteolysis within lysosomes. Increased activity and expression are strongly associated with many pathological processes, including cancers Homo sapiens