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Literature summary for 3.4.24.35 extracted from
- Design of barbiturate-nitrate hybrids that inhibit MMP-9 activity and secretion (2012), J. Med. Chem., 55, 2154-2162.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-(1,5-dihydroxypentan-3-yl)-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens |  |
| 5-(4-hydroxybutan-2-yl)-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(3-(1-nitrooxy-methyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(4-(1-nitrooxy-ethyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(4-(2-nitrooxy-ethyl)piperazin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(4-(2-nitrooxy-ethyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(bis-(2-nitrooxy-ethyl)-amino)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-(4-phenoxyphenyl)-5-(methyl-(2-nitrooxy-ethyl)-amino)-pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-[3-(hydroxymethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-[4-(2-hydroxyethyl)piperazin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-[4-(2-hydroxyethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| 5-[4-(hydroxymethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | - |
Homo sapiens | |
| additional information | design and synthesis of barbiturate-nitrate hybrids, barbiturate-based MMP inhibitors incorporating a nitric oxide donor/mimetic group, that inhibit MMP-9 activity and secretion, reducing effects on cell viability by inhibitors, overview | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | the enzyme is secreted | Homo sapiens | - |
- |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| Caco-2 cell | - |
Homo sapiens | - |
| fibrocarcinoma cell | - |
Homo sapiens | - |
| HT-1080 cell | - |
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 | ? | - |
? | |
| Gelatin + H2O | - |
Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MMP-9 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000062 | - |
pH 7.5, 37°C | Homo sapiens | 5-[3-(hydroxymethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.0000081 | - |
pH 7.5, 37°C | Homo sapiens | 5-[4-(2-hydroxyethyl)piperazin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000012 | - |
pH 7.5, 37°C | Homo sapiens | 5-[4-(2-hydroxyethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000026 | - |
pH 7.5, 37°C | Homo sapiens | 5-(1,5-dihydroxypentan-3-yl)-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000048 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(methyl-(2-nitrooxy-ethyl)-amino)-pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000091 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(bis-(2-nitrooxy-ethyl)-amino)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000092 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(4-(2-nitrooxy-ethyl)piperazin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000097 | - |
pH 7.5, 37°C | Homo sapiens | 5-[4-(hydroxymethyl)piperidin-1-yl]-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000104 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(3-(1-nitrooxy-methyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000145 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-hydroxybutan-2-yl)-5-(4-phenoxyphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000152 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(4-(1-nitrooxy-ethyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | |
| 0.000202 | - |
pH 7.5, 37°C | Homo sapiens | 5-(4-phenoxyphenyl)-5-(4-(2-nitrooxy-ethyl)piperidin-1-yl)-pyrimidine-2,4,6(1H,3H,5H)-trione | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | inhibition of MMP activity, especially MMP-9, has the potential to inhibit tumor growth and metastasis | Homo sapiens |
| physiological function | MMPs can promote cancer cell invasion by degradation of various extracellular matrix components resulting in release of growth factor and cytokines | Homo sapiens |
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