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Literature summary extracted from

  • Cudic, M.; Burstein, G.D.; Fields, G.B.; Lauer-Fields, J.
    Analysis of flavonoid-based pharmacophores that inhibit aggrecanases (ADAMTS-4 and ADAMTS-5) and matrix metalloproteinases through the use of topologically constrained peptide substrates (2009), Chem. Biol. Drug Des., 74, 473-482.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.B12 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol i.e. piceatannol Sus scrofa
3.4.24.B12 pyrogallol
-
 Sus scrofa
3.4.24.82 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol i.e. piceatannol Sus scrofa
3.4.24.82 pyrogallol
-
 Sus scrofa

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.24.82 0.035
-
 Lys(carboxyfluorescein)-Asp-Val-Gln-Glu-Phe-Arg-Gly-Val-Thr-Ala-Val-Ile-Arg-Lys(tetramethylrhodamine)-Lys-Gly-Lys-NH2 pH 7.5, 37°C Sus scrofa

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.B12 Sus scrofa
-
-
-
3.4.24.82 Sus scrofa
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.B12 C6-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-Gly-Thr-Lys(Mca)-Gly-Glu-Leu-Glu-Gly-Arg-Gly-Thr-Lys(Dnp)-Gly-Ile-Ser-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-NH2 + H2O
-
 Sus scrofa ?
-
 ?
3.4.24.B12 Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 + H2O
-
 Sus scrofa ?
-
 ?
3.4.24.B12 Lys(carboxyfluorescein)-Asp-Val-Gln-Glu-Phe-Arg-Gly-Val-Thr-Ala-Val-Ile-Arg-Lys(tetramethylrhodamine)-Lys-Gly-Lys-NH2 + H2O
-
 Sus scrofa ?
-
 ?
3.4.24.82 Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 + H2O
-
 Sus scrofa ?
-
 ?
3.4.24.82 Lys(carboxyfluorescein)-Asp-Val-Gln-Glu-Phe-Arg-Gly-Val-Thr-Ala-Val-Ile-Arg-Lys(tetramethylrhodamine)-Lys-Gly-Lys-NH2 + H2O
-
 Sus scrofa ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.24.B12 ADAMTS-5
-
 Sus scrofa
3.4.24.B12 aggrecanase-2
-
 Sus scrofa
3.4.24.82 ADAMTS-4
-
 Sus scrofa
3.4.24.82 aggrecanase-1
-
 Sus scrofa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.24.B12 0.0012
-
 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol pH 7.5, 37°C, substrate: C6-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-Gly-Thr-Lys(7-methoxycoumarin-4-yl)-Gly-Glu–Leu–Glu–Gly-Arg–Gly-Thr-Lys(Dnp)-Gly-Ile-Ser-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-NH2 Sus scrofa
3.4.24.B12 0.00363
-
 pyrogallol pH 7.5, 37°C, substrate: C6-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-Gly-Thr-Lys(7-methoxycoumarin-4-yl)-Gly-Glu–Leu–Glu–Gly-Arg–Gly-Thr-Lys(Dnp)-Gly-Ile-Ser-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-NH2 Sus scrofa
3.4.24.B12 0.0111
-
 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol pH 7.5, 37°C, substrate: pH 7.5, 37°C, substrate: Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 Sus scrofa
3.4.24.B12 0.037
-
 pyrogallol pH 7.5, 37°C, substrate: Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 Sus scrofa
3.4.24.82 0.00268
-
 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol pH 7.5, 37°C, substrate: C6-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-Gly-Thr-Lys(7-methoxycoumarin-4-yl)-Gly-Glu–Leu–Glu–Gly-Arg–Gly-Thr-Lys(Dnp)-Gly-Ile-Ser-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-NH2 Sus scrofa
3.4.24.82 0.00506
-
 (E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol pH 7.5, 37°C, substrate: pH 7.5, 37°C, substrate: Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 Sus scrofa
3.4.24.82 0.00634
-
 pyrogallol pH 7.5, 37°C, substrate: C6-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-Gly-Thr-Lys(7-methoxycoumarin-4-yl)-Gly-Glu–Leu–Glu–Gly-Arg–Gly-Thr-Lys(Dnp)-Gly-Ile-Ser-(Gly-Pro-Hyp-Pro-Hyp-Gly)2-Gly-Pro-Hyp-NH2 Sus scrofa
3.4.24.82 0.041
-
 pyrogallol pH 7.5, 37°C, substrate: Lys(7-methoxycoumarin-4-yl)-Lys-Gln-Glu-Phe-Arg-Gly-Gln-Thr-Lys(Dnp)-NH2 Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.82 0.005
-
 pH 7.5, 37°C Sus scrofa pyrogallol