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Table 2 Endogenous and exogenous substrates for ABC transporters

From: ABC transporters as multidrug resistance mechanisms and the development of chemosensitizers for their reversal

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
  1. * PMEA, 2',3'-dideoxycytidine 9'-(2'-hosphonylmethoxynyl)adenine