Table 2 Endogenous and exogenous substrates for ABC transporters
Name | Endogenous substrate | Exogenous cytotoxic substance |
|---|---|---|
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 |