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Literature summary extracted from

  • Komiyama, T.; Coppola, J.M.; Larsen, M.J.; van Dort, M.E.; Ross, B.D.; Day, R.; Rehemtulla, A.; Fuller, R.S.
    Inhibition of furin/PC-catalyzed surface and intracellular processing by small molecules (2009), J. Biol. Chem., 284, 15729-15738.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.4.21.75 drug development extensive clinical use, high bioavailability and relatively low toxicity of dicoumarols suggests that the dicoumarol structure will be a good starting point for development of drug-like inhibitors of furin and other proprotein convertases that can act both intracellularly and at the cell surface Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.75 plasmid pEFGRAPfurin expressed in CHO cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.B25 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid
-
 Rattus norvegicus
3.4.21.B25 3,3',3'',3'''-(benzene-1,4-diyldimethanetriyl)tetrakis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.B25 3,3'-(1,3-benzodioxol-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.B25 3,3'-(2,3-dihydro-1H-inden-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.75 (E)-N-((E)-5-(2-chloro-5-nitrobenzylidene)-4-oxothiazolidin-2-ylidene)-4-methylbenzenesulfonamide competitive inhibitor Homo sapiens
3.4.21.75 (N'Z,N''Z)-4,4'-oxybis(N'-(2-hydroxybenzylidene)benzenesulfonohydrazide) competitive inhibitor Homo sapiens
3.4.21.75 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid noncompetitive inhibitor Homo sapiens
3.4.21.75 3'-oxo-6a,14a-dihydro-3'H-spiro[dibenzo[c,h]xanthene-7,1'-isobenzofuran]-3,11-diyl diacetate
-
 Homo sapiens
3.4.21.75 3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-((2-bromophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-((2-chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-((3,4,5-trimethoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-((4-isopropoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-(benzo[d][1,3]dioxol-5-ylmethylene)bis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3,3'-methylenebis(4-hydroxy-2H-chromen-2-one) noncompetitive inhibitor Homo sapiens
3.4.21.75 3-(alpha-acetonyl-benzyl)-4-(hydroxycoumarin)
-
 Homo sapiens
3.4.21.75 3-allyl-1-methyl-1,2,3,4-tetrahydroisoquinoline competitive inhibitor Homo sapiens
3.4.21.75 3-hydroxy-5-(4-methoxyphenyl)-2-(4-phenoxy-3-sulfophenyl)-3H-pyrazol-2-ium competitive inhibitor Homo sapiens
3.4.21.75 4-hydroxy-3-oxo-1-phenylbutylcoumarin
-
 Homo sapiens
3.4.21.75 4-Hydroxycoumarin
-
 Homo sapiens
3.4.21.75 6-oxo-6H-benzo[c]chromen-3-yl 2-chlorobenzoate
-
 Homo sapiens
3.4.21.75 methyl 4-(bis(4-hydroxy-2-oxo-2H-chromen-3-yl)methyl)benzoate noncompetitive inhibitor Homo sapiens
3.4.21.75 N''-[(1E)-[2-[(4-chlorobenzyl)oxy]phenyl]methylidene]carbonohydrazonic diamide competitive inhibitor Homo sapiens
3.4.21.75 N-(benzo[d][1,3]dioxol-5-yl)-1,2,3,4-tetrahydroacridin-9-amine competitive inhibitor Homo sapiens
3.4.21.75 N-(thiazol-2-yl)-4-(5-((2,4,6-trioxotetrahydropyrimidin-5(6H)-ylidene)methyl)furan-2-yl)benzenesulfonamide competitive inhibitor Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.75 0.0123
-
 Ac-Arg-Val-Arg-Arg-4-nitroanilide
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.75 cell surface
-
 Homo sapiens 9986
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.B25 Rattus norvegicus Q78EH2
-
-
3.4.21.75 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.75
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.75 Ac-Arg-Val-Arg-Arg-4-nitroanilide + H2O
-
 Homo sapiens Ac-Arg-Val-Arg-Arg + 4-nitroaniline
-
 ?
3.4.21.75 anthrax protective antigen precursor + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.75 CPA95 + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.75 membrane-type 1-matrix metalloproteinase + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.75 N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumarin 7-amide + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.75 Proprotein convertase
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.B25 0.0083
-
 3,3',3'',3'''-(benzene-1,4-diyldimethanetriyl)tetrakis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.B25 0.012
-
 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid
-
 Rattus norvegicus
3.4.21.B25 0.013
-
 3,3'-(2,3-dihydro-1H-inden-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.B25 0.014
-
 3,3'-(1,3-benzodioxol-5-ylmethanediyl)bis(4-hydroxy-2H-chromen-2-one)
-
 Rattus norvegicus
3.4.21.75 0.00104
-
 3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one) with CPA95 as substrate Homo sapiens
3.4.21.75 0.0033
-
 3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one) with CPA95 as substrate Homo sapiens
3.4.21.75 0.00605
-
 3,3'-(benzo[d][1,3]dioxol-5-ylmethylene)bis(4-hydroxy-2H-chromen-2-one) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.0118
-
 N''-[(1E)-[2-[(4-chlorobenzyl)oxy]phenyl]methylidene]carbonohydrazonic diamide with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.012
-
 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid with CPA95 as substrate/with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens
3.4.21.75 0.0188
-
 3,3'-methylenebis(4-hydroxy-2H-chromen-2-one) with CPA95 as substrate Homo sapiens
3.4.21.75 0.0208
-
 3,3'-((4-isopropoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.022
-
 3,3'-((3,4,5-trimethoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.0783
-
 3,3'-((2-chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.1452
-
 methyl 4-(bis(4-hydroxy-2-oxo-2H-chromen-3-yl)methyl)benzoate with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 0.1851
-
 3,3'-((2-bromophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 1.3
-
 4-hydroxy-3-oxo-1-phenylbutylcoumarin with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 2
-
 3-(alpha-acetonyl-benzyl)-4-(hydroxycoumarin) with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens
3.4.21.75 7.3
-
 4-Hydroxycoumarin with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.75 0.004
-
 with CPA95 as substrate Homo sapiens 3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one)
3.4.21.75 0.007
-
 with CPA95 as substrate/with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid
3.4.21.75 0.011
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens N-(thiazol-2-yl)-4-(5-((2,4,6-trioxotetrahydropyrimidin-5(6H)-ylidene)methyl)furan-2-yl)benzenesulfonamide
3.4.21.75 0.02
-
 with CPA95 as substrate Homo sapiens 3,3'-methylenebis(4-hydroxy-2H-chromen-2-one)
3.4.21.75 0.025
-
 with CPA95 as substrate Homo sapiens 3'-oxo-6a,14a-dihydro-3'H-spiro[dibenzo[c,h]xanthene-7,1'-isobenzofuran]-3,11-diyl diacetate
3.4.21.75 0.028
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens 6-oxo-6H-benzo[c]chromen-3-yl 2-chlorobenzoate
3.4.21.75 0.051
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens 3-allyl-1-methyl-1,2,3,4-tetrahydroisoquinoline
3.4.21.75 0.055
-
 with CPA95 as substrate Homo sapiens 3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one)
3.4.21.75 0.084
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens (N'Z,N''Z)-4,4'-oxybis(N'-(2-hydroxybenzylidene)benzenesulfonohydrazide)
3.4.21.75 0.102
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens (E)-N-((E)-5-(2-chloro-5-nitrobenzylidene)-4-oxothiazolidin-2-ylidene)-4-methylbenzenesulfonamide
3.4.21.75 0.137
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens 3-hydroxy-5-(4-methoxyphenyl)-2-(4-phenoxy-3-sulfophenyl)-3H-pyrazol-2-ium
3.4.21.75 0.159
-
 with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate Homo sapiens N-(benzo[d][1,3]dioxol-5-yl)-1,2,3,4-tetrahydroacridin-9-amine