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Literature summary extracted from

  • Moroy, G.; Denhez, C.; El Mourabit, H.; Toribio, A.; Dassonville, A.; Decarme, M.; Renault, J.H.; Mirand, C.; Bellon, G.; Sapi, J.; Alix, A.J.; Hornebeck, W.; Bourguet, E.
    Simultaneous presence of unsaturation and long alkyl chain at P1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies (2007), Bioorg. Med. Chem., 15, 4753-4766.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.24.24 additional information activation of pro-MMP-2 by 4-aminophenylmercuric acetate Homo sapiens
3.4.24.35 additional information activation of pro-MMP-9 by 4-aminophenylmercuric acetate Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.24 (2E)-3-(N-hydroxycarbamoyl)-2-(3-phenylpropylidene)propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.24 (2E)-3-(N-hydroxycarbamoyl)-2-heptylidenepropionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.24 (2E)-3-(N-hydroxycarbamoyl)-2-isopropionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.24 (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-3-phenylprop-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.24 (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-but-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.24 ilomastat
-
 Homo sapiens
3.4.24.24 additional information inhibitor synthesis and molecular docking, overview Homo sapiens
3.4.24.35 (2E)-3-(N-hydroxycarbamoyl)-2-(3-phenylpropylidene)propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.35 (2E)-3-(N-hydroxycarbamoyl)-2-heptylidenepropionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.35 (2E)-3-(N-hydroxycarbamoyl)-2-isopropionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.35 (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-3-phenylprop-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.35 (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-but-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
-
 Homo sapiens
3.4.24.35 ilomastat
-
 Homo sapiens
3.4.24.35 additional information inhibitor synthesis and molecular docking, overview Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.24.24 Zn2+
-
 Homo sapiens
3.4.24.35 Zn2+
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.24 Homo sapiens
-
-
-
3.4.24.35 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.24.24 additional information activation of pro-MMP-2 by 4-aminophenylmercuric acetate Homo sapiens
3.4.24.35 additional information activation of pro-MMP-2 by 4-aminophenylmercuric acetate Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.24.24 commercial preparation recombinant pro-MMP-2 Homo sapiens
-
3.4.24.35 commercial preparation recombinant pro-MMP-9 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.24 (7-methoxycoumarin-4-yl)acetyl-L-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 + H2O a quenched fluorogenic substrate Homo sapiens ?
-
 ?
3.4.24.35 2,4-dinitrophenyl-Pro-beta-cyclohexylalanyl-Gly-Cys(Me)-His-Ala-Lys(N-Me-2-aminobenzoyl)-NH2 + H2O a quenched fluorogenic substrate Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.24.24 gelatinase A
-
 Homo sapiens
3.4.24.24 MMP-2
-
 Homo sapiens
3.4.24.35 gelatinase B
-
 Homo sapiens
3.4.24.35 MMP-9
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.24 0.0000011
-
-
 Homo sapiens ilomastat
3.4.24.24 0.0000092
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-isopropionyl-L-tryptophan-N-methylamide
3.4.24.24 0.00012
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-3-phenylprop-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
3.4.24.24 0.000123
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-heptylidenepropionyl-L-tryptophan-N-methylamide
3.4.24.24 0.00028
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-(3-phenylpropylidene)propionyl-L-tryptophan-N-methylamide
3.4.24.24 0.0785
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-but-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
3.4.24.35 0.0000005
-
-
 Homo sapiens ilomastat
3.4.24.35 0.000017
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-isopropionyl-L-tryptophan-N-methylamide
3.4.24.35 0.000038
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-3-phenylprop-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
3.4.24.35 0.000045
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-(3-phenylpropylidene)propionyl-L-tryptophan-N-methylamide
3.4.24.35 0.000974
-
-
 Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-[(2E)-but-2-en-1-ylidene]propionyl-L-tryptophan-N-methylamide
3.4.24.35 0.01
-
 above Homo sapiens (2E)-3-(N-hydroxycarbamoyl)-2-heptylidenepropionyl-L-tryptophan-N-methylamide