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Literature summary for 3.4.21.75 extracted from

  • Podsiadlo, P.; Komiyama, T.; Fuller, R.S.; Blum, O.
    Furin inhibition by compounds of copper and zinc (2004), J. Biol. Chem., 279, 36219-36227.
    View publication on PubMed
Search for more literature for 3.4.21.75

Application

Application Comment Organism
medicine copper and zinc complexes of terpyridine derivatives are stable under various conditions and are not expected to pose delivery problems, qualities vital for the development of a wide-scope anti-bioterror agent for civil and military uses Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Cu(2,2':6,2''-terpyridine)Cl2 IC50: 0.0077 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Cu(4'-hydroxo-2,2':6',2''-terpyridine)Cl2 IC50: 0.0072 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Cu(4'-[4-methoxyphenyl]-2,2':6',2''-terpyridine)Cl2 IC50: 0.0051 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Cu(4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2 0.005 mM Homo sapiens
Cu(4,4''-dimethyl-4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2 IC50: 0.014 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Cu(di-[2-picolyl]amine)Cl2 IC50: 0.038 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Cu2+ IC50: 0.014 mM Homo sapiens
Zn(4'-[4-methoxyphenyl]-2,2':6',2''-terpyridine)Cl2 IC50: 0.009 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Zn(4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2 IC50: 0.009 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Zn(4,4''-dimethyl-4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2 0.014 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
Zn2+ IC50: 0.021 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens
[Cu(2,2':6,2''-terpyridine)Cl2] (OCl4) IC50: 0.0069 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide + H2O
-
 Homo sapiens tert-butyloxycarbonyl-Arg-Val-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0051
-
 IC50: 0.0051 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Cu(4'-[4-methoxyphenyl]-2,2':6',2''-terpyridine)Cl2
0.0069
-
 IC50: 0.0069 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens [Cu(2,2':6,2''-terpyridine)Cl2] (OCl4)
0.0072
-
 IC50: 0.0072 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Cu(4'-hydroxo-2,2':6',2''-terpyridine)Cl2
0.0077
-
 IC50: 0.0077 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Cu(2,2':6,2''-terpyridine)Cl2
0.009
-
 IC50: 0.009 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Zn(4'-[4-methoxyphenyl]-2,2':6',2''-terpyridine)Cl2
0.009
-
 IC50: 0.009 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Zn(4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2
0.014
-
 IC50: 0.014 mM Homo sapiens Cu2+
0.014
-
 IC50: 0.014 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Cu(4,4''-dimethyl-4'-[p-tolyl]-2,2':6',2''-terpyridine)Cl2
0.021
-
 IC50: 0.021 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Zn2+
0.038
-
 IC50: 0.038 mM, irreversible, competitive with substrate tert-butyloxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumaryl-7-amide Homo sapiens Cu(di-[2-picolyl]amine)Cl2