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Literature summary for 7.6.2.2 extracted from
- Transition state analysis of the coupling of drug transport to ATP hydrolysis by P-glycoprotein (2003), J. Biol. Chem., 278, 52629-52640.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | Pgp plays a central role in compromising cancer chemotherapy and in modulating the bioavailability and distribution of therapeutic agents | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| MDR1 gene, expression in Saccharomyces cerevisiae | Homo sapiens |
| pgp1 gene, expression in Chinese hamster ovary CR1R12 cells | Cricetulus griseus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetic data, kinetic model of drug transport | Cricetulus griseus | |
| additional information | - |
additional information | kinetic data, kinetic model of drug transport | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| plasma membrane | - |
Cricetulus griseus | 5886 | - |
| plasma membrane | recombinant Pgp, expressed in Saccharomyces cerevisiae | Homo sapiens | 5886 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | Pgp transports drugs out of cells | ? | - |
? |  |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Cricetulus griseus | - |
- |
- |
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Cricetulus griseus |
| recombinant Pgp | Homo sapiens |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| ATP + H2O + xenobiotic[side 1] = ADP + phosphate + xenobiotic[side 2] | thermodynamic data of ATP hydrolysis, mechanism | Cricetulus griseus | |
| ATP + H2O + xenobiotic[side 1] = ADP + phosphate + xenobiotic[side 2] | thermodynamic data of ATP hydrolysis, mechanism | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| ovary | - |
Cricetulus griseus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in | Hoechst 33342 | Homo sapiens | ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out | - |
? | |
| ATP + H2O + colchicine/in | - |
Homo sapiens | ADP + phosphate + colchicine/out | - |
? | |
| ATP + H2O + rhodamine 123/in | - |
Homo sapiens | ADP + phosphate + rhodamine 123/out | - |
? | |
| ATP + H2O + valinomycin/in | - |
Cricetulus griseus | ADP + phosphate + valinomycin/out | - |
? | |
| ATP + H2O + valinomycin/in | - |
Homo sapiens | ADP + phosphate + valinomycin/out | - |
? | |
| ATP + H2O + verapamil/in | - |
Cricetulus griseus | ADP + phosphate + verapamil/out | - |
? | |
| ATP + H2O + verapamil/in | unlabeled and spin-labeled verapamil | Homo sapiens | ADP + phosphate + verapamil/out | - |
? | |
| ATP + H2O + vinblastine/in | - |
Homo sapiens | ADP + phosphate + vinblastine/out | - |
? | |
| ATP + H2O + xenobiotic/in | Pgp transports drugs out of cells, very broad specificity drug pump, thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism, model of drug transport | Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
| ATP + H2O + xenobiotic/in | thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism | Cricetulus griseus | ADP + phosphate + xenobiotic/out | - |
? | |
| additional information | Pgp transports drugs out of cells | Homo sapiens | ? | - |
? | |
| additional information | ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited, the basal ATPase activity is not a consequence of transport of an endogenous lipid or other substrate, but rather an intrinsic mechanistic property of enzyme | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ABCB1 | - |
Homo sapiens |
| MDR1 | - |
Homo sapiens |
| P-glycoprotein | - |
Homo sapiens |
| PGP1 | - |
Cricetulus griseus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 35 | 37 | assay at | Cricetulus griseus |
| 35 | 37 | assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | - |
Cricetulus griseus | |
| additional information | - |
additional information | - |
Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | 7.5 | assay at | Cricetulus griseus |
| 7.4 | 7.5 | assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | data for drug inhibition of the basal ATPase activity | Homo sapiens |
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