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Literature summary for 3.4.24.82 extracted from
- Aggrecanase: The family and its inhibitors (2005), Curr. Med. Chem. Anti-Inflamm. Anti-Allergy, 4, 251-264.
No PubMed abstract available
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| AG3340 | non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 120 nM | Bos taurus |  |
| alpha2-Macroglobulin | - |
Bos taurus | |
| BB-16 | peptidomimetric hydroxamate, synthetic inhibitor originally targeted for matrix metalloproteinases, IC50: 150 nM | Bos taurus | |
| chondroitin 6-sulfate | - |
Bos taurus | |
| dermatan sulfate | - |
Bos taurus | |
| DPC | non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 10 nM | Bos taurus | |
| enoxaparin | - |
Bos taurus | |
| fibronectin | IC50: 110 nM | Bos taurus | |
| heparan sulfate | - |
Bos taurus | |
| heparin | - |
Bos taurus | |
| Keratan sulfate | - |
Bos taurus | |
| marimastat | IC50: 210 nM | Bos taurus | |
| SE206 | macrocyclic derivate of BB-16, IC50: 76 nM | Bos taurus | |
| tinzaparin | - |
Bos taurus | |
| tissue inhibitor of matrix metalloproteinases-3 | TIMP-3 | Bos taurus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| Macro S strong cation exchange and gelatin-agarose affinity column chromatography | Bos taurus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| cartilage | - |
Bos taurus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| aggrecan + H2O | - |
Bos taurus | fragments of aggrecan | - |
? | |
| N-procollagen + H2O | - |
Bos taurus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aggrecanase-1 | - |
Bos taurus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000033 | - |
tissue inhibitor of matrix metalloproteinases-3 | - |
Bos taurus | |
| 0.00002 | - |
tinzaparin | - |
Bos taurus | |
| 0.00008 | - |
enoxaparin | - |
Bos taurus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00001 | - |
non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 10 nM | Bos taurus | DPC | |
| 0.000076 | - |
macrocyclic derivate of BB-16, IC50: 76 nM | Bos taurus | SE206 | |
| 0.00011 | - |
IC50: 110 nM | Bos taurus | fibronectin | |
| 0.00012 | - |
non-peptidomimetric hydroxamate matrix metalloproteinase inhibitor, IC50: 120 nM | Bos taurus | AG3340 | |
| 0.00015 | - |
peptidomimetric hydroxamate, synthetic inhibitor originally targeted for matrix metalloproteinases, IC50: 150 nM | Bos taurus | BB-16 | |
| 0.00021 | - |
IC50: 210 nM | Bos taurus | marimastat | |
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