Substrates for ABC transporters
Substrates of the various transporter isoforms were identified using in vitro transport studies of human or rodent isoforms or from in vivo studies using knockout mice or mutant rats. A number of substrates are provided. Not all substrates are included in this list.
| MDR1 | Actinomycin D, amitriptyline, cerivastatin, colchicine, cyclosporine A, daunorubicin, digoxin, diltiazem, docetaxel, domperidone, doxorubicin, erlotinib, erythromycin, etoposide, fexofenadine, imatinib, indinavir, ivermectin, lapatinib, loperamide, losartan, lovastatin, nelfinavir, ondansetron, oseltamivir, paclitaxel, phenytoin, prazosin, quinidine, ritonavir, saquinavir, sparfloxacin, terfenadine, tetracycline, (99m)Tc-tetrofosmin, topotecan, vecuronium, verapamil, vinblastine, vincristine |
| MRP1 | Aflatoxin B1, daunorubicin, S-(2,4-dinitrophenyl)-glutathione, doxorubicin, epirubicin, estradiol-17β-glucuronide, estrone-3-sulfate, etoposide glucuronide, folate, fluo-3, oxidized glutathione, glutathione-conjugated aflatoxin B1, glutathione-conjugated chlorambucil, glutathione-conjugated ethacrynic acid, glutathione-conjugated 4-hydroxynonenal, glutathione-conjugated prostaglandin A, grepafloxacin, leukotrienes C4, D4, and E4 (glutathione-conjugated leukotriene C4), methotrexate, methoxychlor, vincristine |
| MRP2 | Acetaminophen-glucuronide, acetaminophen-sulfate, p-aminohippurate, arsenic-glutathione, bilirubin-glucuronide, BQ-123, diclofenac-glucuronide, S-(2,4-dinitrophenyl)-glutathione, estradiol-17β-glucuronide, ethinylestradiol glucuronide, glutathione-conjugated ethacrynic acid, glutathione-conjugated 4-hydroxynonenal, indinavir, leukotriene C4, methotrexate, morphine-3-glucuronide, ochratoxin A, oxidized and reduced glutathione, PhIP, ritonavir, saquinavir, sulfotaurolithocholic acid, taurine-conjugated cholic acid, taurolithocholate sulfate, vinblastine |
| MRP3 | Acetaminophen-glucuronide, bilirubin, estradiol-17β-glucuronide, ethinylestradiol glucuronide, etoposide, etoposide-glucuronide, folate, glycocholate, leucovorin, methotrexate, morphine-3-glucuronide, morphine-6-glucuronide, resveratrol-glucuronide, taurochenodeoxycholate-3-sulfate, taurocholate, taurolithocholate-3-sulfate |
| MRP4 | Adefovir, p-aminohippurate, bimane-glutathione, cefazolin, ceftizoxime, cholic acid, cyclic AMP and GMP, dehydroepiandrosterone sulfate, edaravone sulfate, estradiol-17β-glucuronide, folate, furosemide, glycine- and taurine-conjugated bile acids, hydrochlorothiazide, irinotecan and its active metabolite, leucovorin, leukotriene B4 and C4, 6-mercaptopurine, methotrexate, prostaglandins E1, E2, and F2α, taurocholate, tenofovir, thromboxane B2, topotecan, urate, zidovudine |
| MRP5 | Adefovir, cadmium chloride, cyclic AMP and GMP, 5-fluorouracil, folate, hyaluronan, 6-mercaptopurine, methotrexate, potassium antimonyl, 6-thioguanine |
| MRP6 | BQ-123, S-(2,4-dinitrophenyl)-glutathione, N-ethylmaleimide glutathione, etoposide, leukotriene C4, teniposide |
| MRP7 | Docetaxel, estradiol-17β-glucuronide, leukotriene C4, paclitaxel, vinblastine, vincristine |
| MRP8 | Cyclic AMP and GMP, dehydroepiandrosterone sulfate, estradiol-17β-glucuronide, estrone-3-sulfate, 5-fluorouracil, folate, glycocholate, leukotriene C4, methotrexate, taurocholate, zalcitabine |
| BCRP | Abacavir, aflatoxin B, albendazole sulfoxide, ciprofloxacin, coumestrol, daidzein, dantrolene, dehydroepiandrosterone sulfate, dipyridamole, edaravone sulfate, enrofloxacin, erlotinib, estradiol-17β-glucuronide, estrone-3-sulfate, etoposide, furosemide, gefitinib, genistein, glyburide, grepafloxacin, hematoporphyrin, Hoechst, hydrochlorothiazide, imatinib, lamivudine, lapatinib, methotrexate, mitoxantrone, nitrofurantoin, norfloxacin, ofloxacin, oxfendazole, pheophorbide a, PhIP, prazosin, resveratrol 3-sulfate, resveratrol di-sulfate, riboflavin, rosuvastatin, triamterene, ulifloxacin, zidovudine |
PhIP, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine.