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Literature summary for 7.6.2.2 extracted from
- ATP-dependent transport of lipophilic cytotoxic drugs by membrane vesicles prepared from MRP-overexpressing HL60/ADR cells (1996), Biochemistry, 35, 14003-14011.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| arsenate | competitive inhibitor of daunorubicin transport | Homo sapiens |  |
| azidophenacylglutathione | competitive inhibitor of daunorubicin transport | Homo sapiens | |
| cyclosporin A | weak competitive inhibitor of daunorubicin transport | Homo sapiens | |
| genistein | competitive inhibitor of daunorubicin transport | Homo sapiens | |
| GSH | competitive inhibitor of daunorubicin transport | Homo sapiens | |
| GSSG | competitive inhibitor of daunorubicin transport | Homo sapiens | |
| MK571 | competitive inhibitor of daunorubicin transport | Homo sapiens | |
| PSC833 | weak competitive inhibitor of daunorubicin transport | Homo sapiens | |
| verapamil | weak competitive inhibitor of daunorubicin transport | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0055 | - |
vincristine/in | - |
Homo sapiens | |
| 0.0057 | - |
etoposide/in | - |
Homo sapiens | |
| 0.0061 | - |
daunorubicin/in | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | enzyme confers cellular resistance to a variety of natural product cytotoxic agents | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HEK-293 cell | - |
Homo sapiens | - |
| HL-60 cell | MRP-overexpressing HL60/ADR cells | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| daunorubicin/in + ATP + H2O | - |
Homo sapiens | daunorubicin/out + ADP + phosphate | - |
? | |
| etoposide/in + ATP + H2O | - |
Homo sapiens | etoposide/out + ADP + phosphate | - |
? | |
| additional information | enzyme confers cellular resistance to a variety of natural product cytotoxic agents | Homo sapiens | ? | - |
? | |
| vincristine/in + ATP + H2O | - |
Homo sapiens | vincristine/out + ADP + phosphate | - |
? | |
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