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Literature summary for 7.6.2.2 extracted from
- Functional reconstitution of substrate transport by purified multidrug resistance protein MRP1 (ABCC1) in phospholipid vesicles (2000), J. Biol. Chem., 275, 34166-34172.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| GSH | stimulates transport of vincristine | Homo sapiens |  |
| verapamil | stimulates transport of vincristine | Homo sapiens | |
| vincristine | stimulates transport of GSH | Homo sapiens | |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 17-beta-estradiol 17-beta-(D-glucuronide) | - |
Homo sapiens | |
| GSSG | - |
Homo sapiens | |
| S-decyl-glutathione | competitive | Homo sapiens | |
| vincristine | alone is a very poor inhibitor of transport of leukotriene C4, together with GSH acts as relatively potent competitive inhibitor | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000036 | - |
leukotriene C4/in | - |
Homo sapiens | |
| 0.2 | - |
ATP | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | transmembrane protein | Homo sapiens | 16020 | - |
| plasma membrane | - |
Homo sapiens | 5886 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | MRP1 is an efflux pump, which can transport conjugated organic anions and cotansport vincristine together with GSH | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| H69AR cell | - |
Homo sapiens | - |
| HEK-293 cell | - |
Homo sapiens | - |
| HL-60 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| leukotriene C4/in + ATP + H2O | - |
Homo sapiens | leukotriene C4/out + ADP + phosphate | - |
? | |
| additional information | MRP1 is an efflux pump, which can transport conjugated organic anions and cotansport vincristine together with GSH | Homo sapiens | ? | - |
? | |
| vincristine/in + ATP + H2O | requires cotransport of GSH | Homo sapiens | vincristine/out + ADP + phosphate | - |
? | |
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