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Literature summary for 7.6.2.2 extracted from
- Modulation of anticancer drug-induced P-glycoprotein expression by naringin (2009), Z. Naturforsch. C, 64, 109-116.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| doxorubicin | activates and induces the enzyme | Homo sapiens |  |
| verapamil | activates and induces the enzyme | Homo sapiens | |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| naringin | i.e. 7-[[2-O-(6-deoxy-alpha-L-mannopyra nosyl)-beta-D-glucopyranosyl]oxy]-2,3-dihydro-5-hydroxy-2-(4-hydroxyphenyl)-4H-1-benzo pyran-4-one. Pre-treatment with naringin prior to doxorubicin treatment increases the sensitivity of the enzyme to doxorubicin, naringin inhibits the doxorubicin-stimulated ATPase activity and may interact directly with the transporter. Naringin seems to modulate the in vivo expression of P-gp | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | - |
Homo sapiens | 16020 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + xenobiotic/in | Homo sapiens | - |
ADP + phosphate + xenobiotic/out | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| native enzyme from liver partially by mitochondria, plasma, endoplasmic reticulum and nuclear membrane fragment preparation | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| carcinoma cell | - |
Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.0197 | - |
recombinant enzyme in resence of naringin, ATPase activity | Homo sapiens |
| 0.0204 | - |
recombinant enzyme, ATPase activity | Homo sapiens |
| 0.0265 | - |
recombinant enzyme in presence of verapamil and doxorubicin, ATPase activity | Homo sapiens |
| 0.0268 | - |
recombinant enzyme in presence of verapamil, ATPase activity | Homo sapiens |
| 0.0289 | - |
recombinant enzyme in presence of naringin and doxorubicin, ATPase activity | Homo sapiens |
| 0.0386 | - |
recombinant enzyme in presence of doxorubicin, ATPase activity | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + doxorubicin/in | - |
Homo sapiens | ADP + phosphate + doxorubicin/out | - |
? | |
| ATP + H2O + verapamil/in | - |
Homo sapiens | ADP + phosphate + verapamil/out | - |
? | |
| ATP + H2O + xenobiotic/in | - |
Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| P-glycoprotein | - |
Homo sapiens |
| P-gp | - |
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 |
|---|---|---|---|
| 6.8 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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