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. Author manuscript; available in PMC: 2015 Sep 2.
Published in final edited form as: Drug Metab Rev. 2013 Feb;45(1):48–59. doi: 10.3109/03602532.2012.748793

Table 2.

Enterohepatic localization, transporter function, gene and corresponding protein name, and NRs that regulate the drug and bile-acid efflux transporters discussed in this review.

Gene Protein Function Endogenous substrates Exogenous substrates Enterohepatic location NR regulators
ABCB1 MDR1/P-gp ATP-dependent efflux Vinblastine, paclitaxel, doxorubicin, etoposide, verapamil, digoxin, cyclosporine A (Klaassen and Lu, 2008), antiepileptics (Zhang et al., 2012), rifampicin, dexamethasone, and ritonavir (Cascorbi, 2011). For complete list, see Cheng and Klaassen (2006) Apical membrane of enterocytes and hepatocytes (Klaassen and Lu, 2008; Cascorbi, 2011) PXR
VDR
CAR
OSTα/OSTβ OSTα/OSTβ Efflux Bile acids (Dawson et al., 2005). estrone 3-sulfate, and prostaglandins (Klaassen and Aleksunes, 2010) Digoxin (Klaassen and Aleksunes, 2010) Basolateral membrane of hepatocytes and enterocytes (Klaassen and Lu, 2008) FXR
VDR
ABCC2 MRP2 Efflux Bilirubin, leukotriene C4, estrone 3-sulfate, and cholecystokinin (Keppler, 2011) Ochratoxin A (Keppler, 2011), anthracyclines, Vinca alkaloids, methotrexate, and HIV protease inhibitors (Meijerman et al., 2008) Apical membrane of hepatocyte and enterocyte (Klaassen and Lu, 2008) PXR
FXR
CAR
ABCC3 MRP3 Efflux leukotriene C4, bilirubin, dehydroepiandrosterone 3-sulfate, and cholylglycine (Keppler, 2011) bile acids Methotrexate, etopiside, taniposide, and epipodophyllotoxins (Meijerman et al., 2008) Basolateral membrane of enterocytes and hepatocytes (Klaassen and Lu, 2008) PXR
FXR
CAR
ABCC4 MRP4 Efflux Leukotrienes, Prostaglandins, Thromboxane B2, dehydroepiandrosterone 3-sulfate, and conjugated bile salts (Keppler, 2011) Nucleotide analogs and methotrexate (Meijerman et al., 2008) Basolateral membrane of hepatocytes (Klaassen and Lu, 2008) CAR
ABCG2 BCRP Efflux dehydroepiandrosterone sulfate, estradiol-17β-glucuronide, and estrone 3-sulfate (Klaassen and Aleksunes, 2010) Fluoroquinolones, statins, anticancer agents, and furosemide. For complete list, see Denson et al. (2001) Apical membrane of hepatocytes and enterocytes (Klaassen and Lu, 2008) PXR
CAR
ABCB11 BSEP Efflux Conjugated and unconjugated bile acids Apical membrane of hepatocytes (Klaassen and Lu, 2008) FXR

Also included are some (not all) substrates of each transporter.