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Literature summary extracted from

  • Liu, R.; Trzaskos, J.M.
    Aggrecanase: The family and its inhibitors (2005), Curr. Med. Chem. Anti-Inflamm. Anti-Allergy, 4, 251-264.
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.82 AG3340 non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 120 nM Bos taurus
3.4.24.82 alpha2-Macroglobulin
-
 Bos taurus
3.4.24.82 BB-16 peptidomimetric hydroxamate, synthetic inhibitor originally targeted for matrix metalloproteinases, IC50: 150 nM Bos taurus
3.4.24.82 chondroitin 6-sulfate
-
 Bos taurus
3.4.24.82 dermatan sulfate
-
 Bos taurus
3.4.24.82 DPC non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 10 nM Bos taurus
3.4.24.82 enoxaparin
-
 Bos taurus
3.4.24.82 fibronectin IC50: 110 nM Bos taurus
3.4.24.82 heparan sulfate
-
 Bos taurus
3.4.24.82 heparin
-
 Bos taurus
3.4.24.82 Keratan sulfate
-
 Bos taurus
3.4.24.82 marimastat IC50: 210 nM Bos taurus
3.4.24.82 SE206 macrocyclic derivate of BB-16, IC50: 76 nM Bos taurus
3.4.24.82 tinzaparin
-
 Bos taurus
3.4.24.82 tissue inhibitor of matrix metalloproteinases-3 TIMP-3 Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.82 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.24.82 Macro S strong cation exchange and gelatin-agarose affinity column chromatography Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.24.82 cartilage
-
 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.82 aggrecan + H2O
-
 Bos taurus fragments of aggrecan
-
 ?
3.4.24.82 N-procollagen + H2O
-
 Bos taurus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.24.82 aggrecanase-1
-
 Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.24.82 0.0000033
-
 tissue inhibitor of matrix metalloproteinases-3
-
 Bos taurus
3.4.24.82 0.00002
-
 tinzaparin
-
 Bos taurus
3.4.24.82 0.00008
-
 enoxaparin
-
 Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.82 0.00001
-
 non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 10 nM Bos taurus DPC
3.4.24.82 0.000076
-
 macrocyclic derivate of BB-16, IC50: 76 nM Bos taurus SE206
3.4.24.82 0.00011
-
 IC50: 110 nM Bos taurus fibronectin
3.4.24.82 0.00012
-
 non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 120 nM Bos taurus AG3340
3.4.24.82 0.00015
-
 peptidomimetric hydroxamate, synthetic inhibitor originally targeted for matrix metalloproteinases, IC50: 150 nM Bos taurus BB-16
3.4.24.82 0.00021
-
 IC50: 210 nM Bos taurus marimastat