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Literature summary for 7.6.2.1 extracted from
- Interaction of the P-glycoprotein multidrug efflux pump with cholesterol: effects on ATPase activity, drug binding and transport (2008), Biochemistry, 47, 13686-13698.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| cholesterol | the transport activity of P-glycoprotein is elevated by about 40% cholesterol | Cricetulus griseus |  |
| verapamil | a P-glycoprotein modulator known to stimulate ATPase activity in a biphasic manner at micromolar concentrations | Cricetulus griseus | |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| cholesterol | the transport activity of P-glycoprotein decreases by about 20% cholesterol | Cricetulus griseus | |
| methyl-beta-cyclodextrin | transport of 0.001 mM tetramethylrosamine is essentially abolished by 1 mM methyl-beta-cyclodextrin, and transport of 0.005 mM H33342 is almost completely inhibited by 5 mM methyl-beta-cyclodextrin | Cricetulus griseus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| plasma membrane | - |
Cricetulus griseus | 5886 | - |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Cricetulus griseus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| concanavalin A-Sepharose 4B affinity column chromatography and Sephadex G50 gel filtration | Cricetulus griseus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| CHRB30 cell | - |
Cricetulus griseus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + H33342/out | - |
Cricetulus griseus | ADP + phosphate + H33342/in | - |
? | |
| ATP + H2O + phosphatidylcholine/out | - |
Cricetulus griseus | ADP + phosphate + phosphatidylcholine/in | - |
? | |
| ATP + H2O + tetramethylrosamine/out | - |
Cricetulus griseus | ADP + phosphate + tetramethylrosamine/in | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ABCB1 | - |
Cricetulus griseus |
| P-glycoprotein | functions as an ATP-powered multidrug efflux pump for amphipathic molecules | Cricetulus griseus |
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