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Literature summary for 3.4.24.80 extracted from
- Unveiling the surface epitopes that render tissue inhibitor of metalloproteinase-1 inactive against membrane type 1-matrix metalloproteinase (2003), J. Biol. Chem., 278, 40224-40230.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| TIMP-1 mutant forms | TIMP-1(T98L), TIMP-1(V4A), TIMP-1(P6V), TIMP-1(V4S), TIMP-1(P6S), TIMP-1(M66I), TIMP-1(P6A), TIMP-1(M66V), TIMP-1(M66A), TIMP-1(T2S), TIMP-1(M66L), TIMP-1(M66G), TIMP-1(V69L), TIMP-1(M66K), TIMP-1(V4A/P6V/T98L). TIMP-1 is inactive against MT1-MMP. TIMP-1 can be transformed into an active inhibitor against MT1-MMP by the mutation T98L. The resultant mutant displays inhibitory characteristics of a slow, tight binding inhibitor. The potency of the mutant can be further enhanced by the introduction of the mutations V4A and P6V | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | the enzyme regulates extracellular matrix remodeling and is capable of cleaving a wide variety of transmembrane proteins. The enzymatic activity of MT1-MMP is regulated by endogenous inhibitors, TIMP, the tissue inhibitor of metalloproteinases | ? | - |
? |  |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| (7-methoxycoumarin-4-yl)-acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-Ala-Arg-NH2 + H2O | - |
Homo sapiens | (7-methoxycoumarin-4-yl)-acetyl-Pro-Leu-Gly + Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-Ala-Arg-NH2 | - |
? | |
| additional information | the enzyme regulates extracellular matrix remodeling and is capable of cleaving a wide variety of transmembrane proteins. The enzymatic activity of MT1-MMP is regulated by endogenous inhibitors, TIMP, the tissue inhibitor of metalloproteinases | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| membrane type-1 matrix metalloproteinase | - |
Homo sapiens |
| MT1-MPP | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000111 | - |
TIMP-1(T98L) | 27°C | Homo sapiens | |
| 0.000066 | - |
TIMP-1(V4A) | 27°C | Homo sapiens | |
| 0.000078 | - |
TIMP-1(P6V) | 27°C | Homo sapiens | |
| 0.000081 | - |
TIMP-1(V4S) | 27°C | Homo sapiens | |
| 0.000095 | - |
TIMP-1(P6S) | 27°C | Homo sapiens | |
| 0.000146 | - |
TIMP-1(M66I) | 27°C | Homo sapiens | |
| 0.000165 | - |
TIMP-1(P6A) | 27°C | Homo sapiens | |
| 0.000183 | - |
TIMP-1(M66V) | 27°C | Homo sapiens | |
| 0.000199 | - |
TIMP-1(M66A) | 27°C | Homo sapiens | |
| 0.00022 | - |
TIMP-1(T2S) | 27°C | Homo sapiens | |
| 0.000237 | - |
TIMP-1(M66L) | 27°C | Homo sapiens | |
| 0.000254 | - |
TIMP-1(M66G) | 27°C | Homo sapiens | |
| 0.000259 | - |
TIMP-1(V69L) | 27°C | Homo sapiens | |
| 0.000462 | - |
TIMP-1(M66K) | 27°C | Homo sapiens |
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