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REGULATION OF DRUG TRANSPORTERS: DURING INFECTION AND INFLAMMATION
Table 2.
Overview of Transporter Localization and Substrate Chemistry
| Transporter | Tissue localization | Membrane localization | Substrate chemistry | Notes |
|---|---|---|---|---|
| aPFIC, progressive familial intrahepatic cholestasis | ||||
| PGP (ABCB1) | Ubiquitous; high in liver, kidney, gut, brain, testis, placenta | Apical | Numerous xenobiotics, large lipophilic cations or uncharged compounds | Involved in multidrug resistance |
| MDR2 (ABCB4) | Liver | Apical | Phosphatidylcholine,cholesterol | Mutations lead to PFICa type 3 |
| BSEP (ABCB11) | Liver, placenta | Apical | Bile acids, limited xenobiotic transport | Mutations lead to PFIC type 2 |
| MRP1 (ABCC1) | Ubiquitous, low in liver | Basolateral | Amphipathic organic anions, lipophilic drugs and glutathione, sulfate or glucuronate-conjugated compounds | Involved in multidrug resistance |
| MRP2 (ABCC2) | Liver, gut, kidney, brain,placenta, gall bladder | Apical | Many drugs, bile acids, bilirubin, leukotriene, glucuronide and glutathione conjugates | Involved in multidrug resistance; mutations lead to Dubin-Johnson syndrome |
| MRP3 (ABCC3) | Liver, gut, brain, kidney, prostate, pancreas, gall bladder, lung and placenta | Basolateral | Bile acids, bilirubin, 17β-glucuronosyl estradiol, leukotriene, glucuronide conjugates of drugs | Expression is induced in Dubin-Johnson patients and during cholestasis |
| BCRP (ABCG2) | Placenta, liver, kidney, intestine, brain | Apical | Numerous drugs, particularly antineoplastics, estrogen | Involved in multidrug resistance |
| OATP1 (SLC21a1) | Liver, kidney, brain, lung, colon | Basolateral | Bromosulfophthalein, bile acids, steroids, eukotriene | Bi-directional transport; Mediates sodium-independent bile acid uptake |
| OATP2 (SLC21a5) | Liver, kidney, brain, retina, heart, lung, spleen, skeletal muscle, testis | Basolateral | Many anionic compounds, estrogen, bilirubin, steroids, bile acids, glucuronide conjugates, GSH | Bi-directional transport; mediates sodium-independent bile acid upake |
| NTCP (SLC10a1) | Liver | Basolateral | Conjugated bile salts, estrone-3-sulfate, dehydroepiandrosterone sulfate, bromo-sulfophthalein | Mediates sodium-dependent bile acid uptake |
