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Literature summary for 7.6.2.2 extracted from
- Effects of chemopreventive citrus phytochemicals on human P-glycoprotein and multidrug resistance protein 1 (2008), Eur. J. Pharmacol., 600, 45-49.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| auraptene | stimulates the ATPase activity of MRP1. No inhibition of MRP1-mediated efflux by auraptene, but auraptene increases the accumulation of daunorubicin in KB-C2 cells | Homo sapiens |  |
| nobiletin | a chemopreventive citrus phytochemical from orange, stimulates the ATPase activity of MRP1. Nobiletin also increases the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells | Homo sapiens | |
| verapamil | stimulates ATPase activity of P-glycoprotein | Homo sapiens | |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of P-glycoprotein or MRP1 in membranes from Trichoplusia ni High Five cells using the baculovirus transfection system, overexpression of P-glycoprotein in human carcinoma KB-C2 cells, overexpression of MRP1 in human KB/MRP cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| auraptene | stimulates the ATPase activity of MRP1. No inhibition of MRP1-mediated efflux by auraptene, but auraptene increases the accumulation of daunorubicin in KB-C2 cells | Homo sapiens | |
| indomethacin | an inhibitor of MRP1 | Homo sapiens | |
| MK-571 | an inhibitor of MRP1 | Homo sapiens | |
| nobiletin | a chemopreventive citrus phytochemical from orange, stimulates the ATPase activity of MRP1. Nobiletin also increases the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells, and of P-glycoprotein substrate daunorubicin in KB-C2 cells | 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 + calcein/in | Homo sapiens | fluorescent substrate of MRP1 | ADP + phosphate + calcein/out | - |
? | |
| ATP + H2O + daunorubicin/in | Homo sapiens | fluorescent substrate of P-glycoprotein | ADP + phosphate + daunorubicin/out | - |
? | |
| ATP + H2O + xenobiotic/in | Homo sapiens | - |
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 + calcein/in | fluorescent substrate of MRP1 | Homo sapiens | ADP + phosphate + calcein/out | - |
? | |
| ATP + H2O + daunorubicin/in | fluorescent substrate of P-glycoprotein | Homo sapiens | ADP + phosphate + daunorubicin/out | - |
? | |
| ATP + H2O + xenobiotic/in | - |
Homo sapiens | ADP + phosphate + xenobiotic/out | - |
? | |
| additional information | P-glycoprotein seems to prefer amphipathic cationic compounds, and MRP1 anionic compounds | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ABCB1 | - |
Homo sapiens |
| ABCC1 | - |
Homo sapiens |
| MRP1 | - |
Homo sapiens |
| multidrug resistance protein 1 | - |
Homo sapiens |
| P-glycoprotein | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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