EC Number | Activating Compound | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.1 | cholesterol | the transport activity of P-glycoprotein is elevated by about 40% cholesterol | Cricetulus griseus | |
7.6.2.1 | verapamil | a P-glycoprotein modulator known to stimulate ATPase activity in a biphasic manner at micromolar concentrations | Cricetulus griseus |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.1 | cholesterol | the transport activity of P-glycoprotein decreases by about 20% cholesterol | Cricetulus griseus | |
7.6.2.1 | 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 | |
7.6.2.2 | cholesterol | presence of cholesterol in the bilayer modulates the basal and drug-stimulated ATPase activity of reconstituted Pgp in vesicles. Both the ability of drugs to bind to the protein and the drug transport and phospholipid flippase functions of Pgp are also affected by cholesterol. The effects of cholesterol on drug binding affinity are unrelated to the size of the compound. Increasing cholesterol content greatly alters the partitioning of hydrophobic drug substrates into the membrane, which may account for some of the effects of cholesterol on Pgp-mediated drug transport | Cricetulus griseus | |
7.6.2.2 | methyl-beta-cyclodextrin | over 85% inhibition of ATPase at 10 mM, about 55% inhibition of the lipid flippase at 10 mM | Cricetulus griseus |
EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
7.6.2.2 | additional information | - |
additional information | dissociation constants of transported substrates, effect of cholesterol on ATP and drug binding to reconstituted Pgp, overview | Cricetulus griseus |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
7.6.2.1 | plasma membrane | - |
Cricetulus griseus | 5886 | - |
7.6.2.2 | cell surface | of tumor cells | Cricetulus griseus | 9986 | - |
7.6.2.2 | plasma membrane | - |
Cricetulus griseus | 5886 | - |
EC Number | Metals/Ions | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.2 | Mg2+ | - |
Cricetulus griseus |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
7.6.2.2 | ATP + H2O + xenobiotic/in | Cricetulus griseus | expression at the tumor cell surface of P-glycoprotein, which functions as an ATP-powered multidrug efflux pump, is involved in multidrug resistance. It also shows lipid flippase activity | ADP + phosphate + xenobiotic/out | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
7.6.2.1 | Cricetulus griseus | - |
- |
- |
7.6.2.2 | Cricetulus griseus | - |
- |
- |
EC Number | Purification (Comment) | Organism |
---|---|---|
7.6.2.1 | concanavalin A-Sepharose 4B affinity column chromatography and Sephadex G50 gel filtration | Cricetulus griseus |
7.6.2.2 | native P-gp by CHAPS-mediated extraction from plasma membrane, followed by concanavalin A affinity chromatography. Reconstitution in lipid proteoliposomes, that are further purified by gel filtration | Cricetulus griseus |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
7.6.2.1 | CHRB30 cell | - |
Cricetulus griseus | - |
7.6.2.2 | carcinoma cell | - |
Cricetulus griseus | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
7.6.2.1 | ATP + H2O + H33342/out | - |
Cricetulus griseus | ADP + phosphate + H33342/in | - |
? | |
7.6.2.1 | ATP + H2O + phosphatidylcholine/out | - |
Cricetulus griseus | ADP + phosphate + phosphatidylcholine/in | - |
? | |
7.6.2.1 | ATP + H2O + tetramethylrosamine/out | - |
Cricetulus griseus | ADP + phosphate + tetramethylrosamine/in | - |
? | |
7.6.2.2 | ATP + H2O + daunorubicin/in | - |
Cricetulus griseus | ADP + phosphate + daunorubicin/out | - |
? | |
7.6.2.2 | ATP + H2O + H33342/in | - |
Cricetulus griseus | ADP + phosphate + H33342/out | - |
? | |
7.6.2.2 | ATP + H2O + progesterone/in | - |
Cricetulus griseus | ADP + phosphate + progesterone/out | - |
? | |
7.6.2.2 | ATP + H2O + rhodamine 123/in | - |
Cricetulus griseus | ADP + phosphate + rhodamine 123/out | - |
? | |
7.6.2.2 | ATP + H2O + tetramethylrosamine/in | - |
Cricetulus griseus | ADP + phosphate + tetramethylrosamine/out | - |
? | |
7.6.2.2 | ATP + H2O + vinblastine/in | - |
Cricetulus griseus | ADP + phosphate + vinblastine/out | - |
? | |
7.6.2.2 | ATP + H2O + xenobiotic/in | - |
Cricetulus griseus | ADP + phosphate + xenobiotic/out | - |
? | |
7.6.2.2 | ATP + H2O + xenobiotic/in | expression at the tumor cell surface of P-glycoprotein, which functions as an ATP-powered multidrug efflux pump, is involved in multidrug resistance. It also shows lipid flippase activity | Cricetulus griseus | ADP + phosphate + xenobiotic/out | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
7.6.2.1 | ABCB1 | - |
Cricetulus griseus |
7.6.2.1 | P-glycoprotein | functions as an ATP-powered multidrug efflux pump for amphipathic molecules | Cricetulus griseus |
7.6.2.2 | P-glycoprotein | - |
Cricetulus griseus |
7.6.2.2 | P-glycoprotein multidrug efflux pump | - |
Cricetulus griseus |
7.6.2.2 | Pgp | - |
Cricetulus griseus |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
7.6.2.2 | 20 | - |
ATP and substrate binding affinity assays at | Cricetulus griseus |
7.6.2.2 | 37 | - |
ATPase assay at | Cricetulus griseus |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
7.6.2.2 | 7.4 | 8.1 | assay at, dependent on the solubility of participating components of the reconstituting proteoliposomes | Cricetulus griseus |
EC Number | Cofactor | Comment | Organism | Structure |
---|---|---|---|---|
7.6.2.2 | ATP | - |
Cricetulus griseus |