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Endogenous and exogenous substrates for ABC transporters |
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| Name |
Endogenous substrate |
Exogenous cytotoxic substance |
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| MDR1 |
Estrogen glucuronide conjugates (estradiol, estriol), endorphin, glutamate, steroids (cortisol, aldosterone, corticosterone), beta-amyloid, 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (generically platelet-activating factor, PAF) |
Anthracyclines (doxorubucin, daunorubicin, epirubicin), actinomycin D, colchicine, podophyllotoxin (etoposide, teniposide), methotrexate (only in carrier-deficient cells), mitomycin C, mitoxantrone, taxenes (paclitaxel, docetaxel), vinca alkaloids (vincristine, vinblastine) |
| MRP1 |
Estradiol-17beta(beta-D-glucuronide) glutathione, glutathione S-conjugate leukoetriene C4, glucuronosyl bilirubin |
Anthracyclines, cochicine, etoposide, heavy metals (arsenite, arsenate, antimonials), vincristine, vinblastine, paclitaxel |
| MRP2 |
Estradiol-17beta(beta-D-glucuronide), glutathione, glutathione S-conjugate Leukoetriene C4, glucuronosyl bilirubin, |
Cisplatin, CPT-11, doxorubicin, etoposide, methotrexate, SN-38, vincristine, vinblastine |
| MRP3 |
S-(2,4-dinitrophenyl)glutathione |
Cisplatin, doxorubicin, etoposide, methotrexate, teniopside, vincristine, |
| MRP4 |
Glucuronide and glutathione conjugates |
Methotrexate, nucleotide analogs, PMEA* |
| MRP5 |
Glutamate and phosphate conjugates |
Doxorubicin, methotrexate, nucleotide analogs, topotecan, |
| MRP6 |
Cyclic nucleotides (cAMP, cGMP), glutathione conjugate |
Doxorubicin, etoposide, teniposide |
| MRP7 |
? |
? |
| MRP8 |
17beta-estradiol-(17-beta-D-glucuronide), leukotriene C4, cyclic nucleotides |
5'-Fluorouracil, 5'-fluoro-2'-deoxyuridine, 5'-fluoro-5'-deoxyuridine, PMEA* |
| BCRP |
Heme or porphyrin |
Anthracyclines, bisantrene, camptothecin, epirubicin, flavopiridol, mitoxantrone, S-38, topotecan |
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* PMEA, 2',3'-dideoxycytidine 9'-(2'-hosphonylmethoxynyl)adenine | ||
Choi Cancer Cell International 2005 5:30 doi:10.1186/1475-2867-5-30 |
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