Table 2.
ABC transporters in human cancers
| Name/ Gene name | Other Names | Genomic Location | Organ/tissue localization | MW (kDa) | Resistance conferred to | Modulators | References |
|---|---|---|---|---|---|---|---|
| MDR1/ ABCB1 | P-gp, GP170, CLCS, ABC20 | 7p21 | Blood-brain barrier, Bone marrow, Placenta, Gut mucosa, Liver, Kidney | 170 | Taxanes, Epipodophyllotoxins, Vinca Alkaloids, Anthracyclines, BCR-ABL TKIs, EGFR TKIs, ALK TKIs (Crizotinib, Ceritinib) | Sapitinib, Ibrutinib, RN486, Erlotinib, Lapatinib, Tariquidar, Elacridar, Zosuquidar | [101, 142–160] |
| BCRP/ ABCG2 | ABCP, MXR1, CD338, ABC15 | 4q22.1 | Placental syncytiotrophoblasts, Small intestine, Epithelial tissue of colon, Canalicular membrane in the liver, Microvessel endothelium of human brain, in the veins and blood vessels | 72 | Nucleoside analogs, Anthracyclines, Flavopiridols, Methotrexate, Methotrexate polyglutamates, E217βG, Camptothecin-derived topoisomerase I inhibitors, GSK1070916, Tivantinib, Pevonedistat, Tozasertib, Barasertib | Erlotinib, Lapatinib, Icotinib | [153, 159, 161–176] |
| PRP/ ABCB6 | DUH13, PSHK2, ABC14 | 2q35.5 | Brain, Retina, Testis, Gall bladder, Intestine | 93.8 | Paclitaxel, 5-FU, Epirubicin, Cyclophosphamide, Daunorubicin, SN-38, Vincristine | Verteporfin, Tomatine HCl, Benzethonium chloride | [177–182] |
| MRP1/ ABCC1 | GS-X, ABC29 | 16p13.1 | Placenta, BBB, Lungs, Testis, Skeletal/Cardiac muscles, Kidney, Intestine | 171.6 | Anthracyclines, Vinca alkaloids, Epipodophyllotoxins, Camptothecins, GSH conjugates, Methotrexate, Mitoxantrone, Imatinib, Arsenite, Colchicine, Flutamide, Betulin, Saquinavir, Ritonavir, Indinavir | Everolimus, GSK1904529A, Rapamycin, Tipifarnib, TAK-733, Delavirdine, Indomethacin, Verapamil | [145, 183–194] |
| MRP2/ ABCC2 | cMOAT, cMRP, ABC30 | 10q24.2 | Placenta, BBB, Lungs, Kidney, Liver, Intestine | 174.2 | LTC4, E217βG, GSH, Taxanes, Anthracyclines, Vinca alkaloids, Methotrexate, Mitoxantrone, Etoposide, Irinotecan, Cisplatin, SN-38, Saquinavir, Ritonavir, Lopinavir, Indinavir | Curcumin, Piperine, Rhinacanthin-C, Probenecid | [59, 195–202] |
| MRP3/ ABCC3 | cMOAT2, MOATD, MLP2, ABC31 | 17q21.33 | Placenta, Colon, Prostate, Kidney, Liver, Small intestine | 169.3 | Glutathione, Bile salts, LTC4, Glucuronide conjugates, DNP-SG, Vincristine | Fidaxomicin, Suramin, Lamivudine, Tenofovir | [203–208] |
| MRP4/ ABCC4 | MOAT-B, ABC32 | 13q32.1 | Blood, Pancreas, Adrenal gland, Prostatea, Kidneya, Livera | 149.5 | cAMPb, cGMPb, Loop diuretics, Cephalosporins, Topotecan, Imatinib, PMEA, 6-MP, 6-TG, Methotrexate, Plant polyphenols, Resveratrol, Quercetin, Adefovir, Ganciclovir, Tenofovir, Zidovudine | Micafungin, Rofecoxib, Indomethacin, Verapamil | [194, 209–217] |
| MRP5/ ABCC5 | SMRP, MOATC, ABC33 | 3q27.1 | Brain, Testis, Skeletal/Cardiac Muscles | 160.6 | cAMPb, cGMPb, Folates, 6-MP, 5-FU, Methotrexate, Stavudine | Zaprinast, Benzbromarone, Sulfinpyrazone, Sildenafil, Sulfinpyrazone | [216, 218–222] |
| MRP6/ ABCC6 | MLP1, MOAT-E, ABC34 | 16p13.11 | Kidney, Liver | 164.9 | Cyclopentapeptide BQ123, Etoposide, Teniposide, Doxorubicin, Daunorubicin, LTC4, n-ethylmaleimide-glutathione | Indomethacin, Benzobromarone | [194, 223–225] |
| MRP7/ ABCC10 | SIMRP7 | 6p21.1 | Brain, Lungs, Testis, Blood, Prostate, Ovary, Kidney | 161.6 | Taxanes, Vinca alkaloids, 2′,3′-dideoxycytidine, AraC, PMEA, Epothilone B, LTC4, E217βG | Nilotinib, Lapatinib, Tandutinib, PD-173074, Tariquidar | [211, 226–237] |
| MRP8/ ABCC11 | EWWD, CFTR | 16q12.1 | Placentaa, Braina, Livera | 154.3 | DHEAS, E1S, E217βG, LTC4, DNP-SG, AraC, 5-FU, Methotrexate, PMEA, 2′,3′ − dideoxycytidine, Adefovir | [194, 238–242] |
aIndicates low levels of expression
bIndicates that inhibition of MRP4 results in impaired cAMP and cGMP transport