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Literature summary extracted from

  • Law, S.; Du, X.; Panwar, P.; Honson, N.S.; Pfeifer, T.; Roberge, M.; Broemme, D.
    Identification of substrate-specific inhibitors of cathepsin K through high-throughput screening (2019), Biochem. J., 476, 499-512 .
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.22.38 medicine cathepsin K is a drug target for skeletal disorders Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.38 (2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
-
 Homo sapiens
3.4.22.38 13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
-
 Homo sapiens
3.4.22.38 3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
-
 Homo sapiens
3.4.22.38 6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
-
 Homo sapiens
3.4.22.38 acetyl-strophanthidin
-
 Homo sapiens
3.4.22.38 ellipticine
-
 Homo sapiens
3.4.22.38 additional information a fluorescence polarization assay is developed to screen 4761 compounds for substrate-specific ectosteric collagenase inhibitors of cathepsin K. A total of 38 compounds are identified that block the collagenase activity without interfering with the hydrolysis of active site substrates such as the synthetic peptide substrate, benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin, and gelatin. The identified inhibitors can be divided into two main classes, negatively charged and polyaromatic compounds which suggest the binding to different ectosteric sites Homo sapiens
3.4.22.38 sclareol
-
 Homo sapiens
3.4.22.38 suramin
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.38 Homo sapiens P43235
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.38 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.22.38 Collagen + H2O
-
 Homo sapiens ?
-
 ?
3.4.22.38 Gelatin + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.38 catK
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.38 0.005
-
 pH 5.5, 25°C, 16.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens suramin
3.4.22.38 0.009
-
 pH 5.5, 25°C, collagenase activity, 1.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens 3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
3.4.22.38 0.0093
-
 pH 5.5, 25°C, 3.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens sclareol
3.4.22.38 0.0143
-
 pH 5.5, 25°C, collagenase activity, 5.4% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens acetyl-strophanthidin
3.4.22.38 0.0195
-
 pH 5.5, 25°C, collagenase activity, 4.9% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens (2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
3.4.22.38 0.075
-
 pH 5.5, 25°C, collagenase activity, 12% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens 6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
3.4.22.38 0.088
-
 pH 5.5, 25°C, 4.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens ellipticine
3.4.22.38 0.186
-
 pH 5.5, 25°C, collagenase activity, 14% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate Homo sapiens 13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium