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Literature summary for 7.6.2.2 extracted from
- A novel electron paramagnetic resonance approach to determine the mechanism of drug transport by P-glycoprotein (2002), J. Biol. Chem., 277, 45688-45694.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| verapamil | spin-labeled, 5fold stimulation of ATPase activity | Homo sapiens |  |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | ATP-driven pumping of a variety of drugs out of cells by P-glycoprotein poses a serious problem to medical therapy | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Saccharomyces cerevisiae | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| EDTA | - |
Homo sapiens | |
| vanadate | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.004 | - |
verapamil | pH 7.4, 37°C, EPR spin-labeled verapamil | Homo sapiens | |
| 0.8 | - |
ATP | pH 7.4, 37°C, MgATP | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| additional information | recombinant P-glycoprotein, expressed in Saccharomyces cerevisiae proteoliposome | Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + xenobiotic/in | Homo sapiens | ATP-driven pumping of a variety of drugs out of cells, multidrug resistance, hydrophobic model of drug transport by P-glycoprotein | ADP + phosphate + xenobiotic/out | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + verapamil/in | EPR spin-labeled verapamil is an excellent transport substrate, the affinity is 10fold higher than for unlabeled verapamil | Homo sapiens | ADP + phosphate + verapamil/out | - |
? | |
| ATP + H2O + xenobiotic/in | ATP-driven pumping of a variety of drugs out of cells, multidrug resistance, hydrophobic model of drug transport by P-glycoprotein | Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
| ATP + H2O + xenobiotic/in | ATP-driven pumping of a variety of drugs out of cells, hydrophobic vacuum cleaner model of drug transport by P-glycoprotein | Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| P-glycoprotein | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 5.8 | - |
verapamil | pH 7.4, 37°C, EPR spin-labeled verapamil | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
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