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Literature summary for 3.4.24.B4 extracted from
- A new class of potent matrix metalloproteinase 13 inhibitors for potential treatment of osteoarthritis: Evidence of histologic and clinical efficacy without musculoskeletal toxicity in rat models (2009), Arthritis Rheum., 60, 2008-2018.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ALS 1-0635 | noncompetitive | Bos taurus | |
| ALS 1-0635 | noncompetitive | Homo sapiens | |
| ALS 1-0635 | noncompetitive | Rattus norvegicus | |
| ilomastat | a broad-spectrum MMP inhibitor | Bos taurus |  |
| ilomastat | a broad-spectrum MMP inhibitor | Homo sapiens | |
| additional information | development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors | Bos taurus | |
| additional information | development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors | Homo sapiens | |
| additional information | development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors. Effect of MMP-13 inhibition on cartilage degradation in the rat medial meniscal tear model of osteoarthritis, overview | Rattus norvegicus | |
| Ro32-3555 | a broad-spectrum MMP inhibitor | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | steady-state kinetics analysis, overview | Homo sapiens | |
| additional information | - |
additional information | steady-state kinetics analysis, overview | Rattus norvegicus | |
| additional information | - |
additional information | steady-state kinetics analysis, overview | Bos taurus |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular matrix | - |
Homo sapiens | 31012 | - |
| extracellular matrix | - |
Rattus norvegicus | 31012 | - |
| extracellular matrix | - |
Bos taurus | 31012 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Rattus norvegicus | MMP-13 causes cartilage degradation | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
- |
- |
| Homo sapiens | - |
- |
- |
| Rattus norvegicus | - |
male Sprague-Dawley IGS rats | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| cartilage | articular | Bos taurus | - |
| cartilage | of knee meniscus | Rattus norvegicus | - |
| cartilage | osteoarthritic | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 + H2O | - |
Homo sapiens | ? | - |
? | |
| MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 + H2O | - |
Rattus norvegicus | ? | - |
? | |
| MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 + H2O | - |
Bos taurus | ? | - |
? | |
| additional information | MMP-13 causes cartilage degradation | Rattus norvegicus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| matrix metalloproteinase 13 | - |
Homo sapiens |
| matrix metalloproteinase 13 | - |
Rattus norvegicus |
| matrix metalloproteinase 13 | - |
Bos taurus |
| MMP-13 | - |
Homo sapiens |
| MMP-13 | - |
Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
| 7.5 | - |
assay at | Rattus norvegicus |
| 7.5 | - |
assay at | Bos taurus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000078 | - |
ALS 1-0635 | pH not specified in the publication, temperature not specified in the publication | Homo sapiens | |
| 0.00000078 | - |
ALS 1-0635 | pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | |
| 0.00000078 | - |
ALS 1-0635 | pH not specified in the publication, temperature not specified in the publication | Bos taurus |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | interleukin-1 and oncostatin M induce MMP-13 expression | up |
| Rattus norvegicus | interleukin-1 and oncostatin M induce MMP-13 expression | up |
| Bos taurus | interleukin-1 and oncostatin M induce MMP-13 expression | up |
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