TABLE 1

ABC transporters involved in anticancer drug resistance (Dean et al., 2001; Szakacs et al., 2006; Moitra et al., 2011)

GeneProteinRoles in Drug ResistanceAnticancer Drug Substrates/Inducers
ABCA2ABC2Drug transportEstramustine, mitoxantrone
ABCA3ABC3Surfactant lipid transporter, lysosomal drug sequestration (Chapuy et al., 2008)Doxorubicin, daunorubicin (Steinbach et al., 2006), imatinib (Chapuy et al., 2009)
ABCB1P-gp/MDR1Drug transportMultiple, including Vinca alkaloids, anthracyclines, etoposide, taxanes, imatinib, irinotecan, methotrexate, mitoxantrone
ABCB4PGY3/MDR3Phosphatidylcholine and drug transport, bile acid secretionVinblastine (Wang et al., 2008), doxorubicin (Turton et al., 2001)
ABCB5ABC19Drug transport5-Fluorouracil (Wilson et al., 2011), doxorubicin (Frank et al., 2005)
ABCB11SPGPBile salt and drug transportPaclitaxel
ABCC1MRP1Drug transportMultiple, including Vinca alkaloids, anthracyclines, etoposide, imatinib, irinotecan, methotrexate, mitoxantrone
ABCC2MRP2Organic anion efflux, drug transportMultiple, including Vinca alkaloids, anthracyclines, etoposide, taxanes, irinotecan, cisplatin, methotrexate, mitoxantrone
ABCC3MRP3Drug transportEtoposide
ABCC4MRP4Nucleoside and drug transportIrinotecan, thiopurines, methotrexate
ABCC5MRP5Nucleoside and drug transportThiopurines, cisplatin, methotrexate
ABCC6MRP6Drug transportAnthracyclines, etoposide, cisplatin, gemcitabine (Ikeda et al., 2011)
ABCC10MRP7Drug transportVinca alkaloids, taxanes
ABCC11MRP8Drug transport5-Fluorouracil
ABCC12MRP9Drug transportNone identified
ABCG2ABCP/BCRP1Toxin efflux, drug transportMultiple, including anthracyclines, etoposide, imatinib, flavopiridol, irinotecan, methotrexate, mitoxantrone
LRPLRPMajor vault transporter protein (Scheffer et al., 1995)AML induction chemotherapy (List et al., 1996; Huh et al., 2006)