ABC Transporter | No. of Transmembrane Domains | Main Tissue Expression | Apical or Basolateral Membrane Localization | Substratesa | References |
---|---|---|---|---|---|
ABCB1 (MDR1 or P-gp) | 2 | Liver, kidney, intestine, brain, testis, adrenal gland, uterus, ovary | Apical | Quinidine, verapamil, celiprolol, talinolol, digoxin, daunorubicin, doxorubicin, vinblastine, etoposide, methotrexate, mitoxantrone, paclitaxel, topotecan, indinavir, nelfinavir, ritonavir, saquinavir | Kartner et al. (1983), Ueda et al. (1987), Pastan et al. (1988), de Lannoy and Silverman (1992), Hendricks et al. (1992), Peters and Roelofs (1992), Karlsson et al. (1993), de Graaf et al. (1996), Sparreboom et al. (1997), Kim et al. (1998), Gramatte and Oertel (1999), Verschraagen et al. (1999), Jones et al. (2001) |
ABCB4 (MDR3) | 2 | Liver | Apical | Vinblastine, paclitaxel, digoxin | Smith et al. (2000) |
ABCB11 (BSEP or SPGP) | 2 | Liver, intestine | Apical | Vinblastine, cyclosporin, rifampicin | Török et al. (1999), Lecureur et al. (2000), Stieger et al. (2000) |
ABCC1 (MRP1) | 3 | Intestine, brain, kidney, lung, testis | Basolateral | Doxorubicin, daunorubicin, vinblastine, vincristine, etoposide, methotrexate, paclitaxel, grepafloxacin | Cole et al. (1992, 1994), Flens et al. (1996), Sharp et al. (1998), Hooijerb et al. (1999), Evers et al. (2000), Tamai et al. (2000), Cherrington et al. (2002) |
ABCC2 (MRP2 or cMOAT) | 3 | Liver, intestine, kidney | Apical | Cisplatin, doxorubicin, etoposide, vincristine, methotrexate, indinavir, ritonavir, saquinavir, adefovir, cidofovir | Schaub et al. (1997), Cui et al. (1999), Hooijberg et al. (1999), Kawabe et al. (1999), Fromm et al. (2000), Miller (2001), Huisman et al. (2002) |
ABCC3 (MRP3) | 3 | Intestine, kidney, liver, pancreas, placenta, colon | Basolateral | Daunorubicin, doxorubicin, vincristine, etoposide, teniposide, methotrexate | Kool et al. (1997), Belinsky et al. (1998), Kool et al. (1999), Zeng et al. (1999), St-Pierre et al. (2000), Zelcer et al. (2001) |
ABCC4 (MRP4) | 2 | Prostate, lung, adrenal gland, ovary, testis | Basolateral and apical (depending on cell type) | Methotrexate, adefovir | Lee et al. (1998), Schuetz et al. (1999), Lee et al. (2000), Chen et al. (2002) |
ABCC5 (MRP5) | 2 | Skeletal muscle, heart, brain | Basolateral | Adefovir | Kool et al. (1997), Belinsky et al. (1998), Wijnholds et al. (2000), Haimeur et al. (2004) |
ABCC6 (MRP6) | 3 | Kidney, liver | Basolateral | Cisplatin, doxorubicin, etoposide, daunorubicin, | Belinsky and Kruh (1999), Bergen et al. (2000), Belinsky et al. (2002) |
ABCC10 (MRP7) | 3 | Heart, skeletal, muscle, spleen, liver | Not determined | Doxorubicin, vinblastine, vincristine, paclitaxel, docetaxel | Kao et al. (2002), Orr et al. (2003), Hopper-Borge et al. (2004) |
ABCC11 (MRP8) | 2 | Breast, testis | Not determined | Purine and pyrimidine nucleotide analogs | Bera et al. (2001) |
ABCC12 (MRP9) | 2 | Breast, testis, brain, ovary, skeletal muscle | Not determined | Not determined | Bera et al. (2002) |
ABCG2 (BCRP) | 1 | Placenta, brain | Apical | Daunorubicin, doxorubicin, etoposide, teniposide, methotrexate, mitoxantrone, topotecan | Doyle et al. (1998), Maliepaard et al. (1999, 2001), Volk et al. (2002), Allen et al. (2003), Volk and Schneider (2003), Wang et al. (2003), Aronica et al. (2005) |
ABCA8 | Not determined | Heart, skeletal muscle, liver | Not determined | Doxorubicin, digoxin | Tsuruoka et al. (2002) |
cMOAT, canalicular multispecific organic anion transporter; BSEP, bile salt export pump; TAP, transporter associated with antigen processing; CFTR, cystic fibrosis transmembrane conductance regulator
↵ a Not an exhaustive list