Overview of selected SLCO transporters
The table was adapted from Ho and Kim (2010) and Konig (2011).
| Gene Symbol | Protein | Normal Tissue Distribution | Cellular Localization | Example Substrates |
|---|---|---|---|---|
| SLCO1A2 (formerly SLC21A3) | OATP1A2 (formerly OATP-A, OATP1) | Brain (blood-brain barrier), kidney, liver, intestine, eye, placenta, prostate, testis | BL (ciliary body epithelia) | Chemotherapy: atrasentan, chemotherapy-bile acid conjugates (i.e., Bamet-R2, Bamet-UD2, chlorambucil taurocholate), docetaxel, imatinib, methotrexate, microcystin-LR |
| AP (kidney, hepatocytes, intestine) | Other: xenobiotics: BSP, deltorphin, fexofenadine, gadolinium dye for MRI, ouabain, rosuvastatin, levofloxacin, DPDPE, rocuronium, saquinavir; endogenous: bile salts, T4, T3, PGE2, E2G, E3S, DHEAS | |||
| SLCO1B1 (formerly SLC21A6) | OATP1B1 (formerly LST-1, OATP-C, OATP2) | Liver, placenta | BL (hepatocytes) | Chemotherapy: daunorubicin, mitoxantrone, atrasentan, chemotherapy-bile acid conjugates (i.e., Bamet-R2, Bamet-UD2), cytarabine, etoposide, flavopiridol, gimatecan, hydroxyurea, methotrexate, microcystin-LR, carboplatin, cisplatin, oxaliplatin, SN-38 (irinotecan active metabolite), sorafenib-β-D-glucuronide, docetaxel, paclitaxel |
| Other: xenobiotics: olmesartan, valsartan, atrasentan, temocaprilat, pitavastatin, pravastatin, cerivastatin, atorvastatin, rosuvastatin, rifampin, caspofungin, enalapril, BSP, phalloidin, troglitazone, bosentan, benzylpenicillin, nafcillin, some cephalosporins; endogenous: bilirubin, bilirubin-glucuronides, GCA, leukotriene C4, DHEAS, thromboxane B2, T4, T3, PGE2, TCA, E2G, E3S | ||||
| SLCO1B3 (formerly SLC21A8) | OATP1B3 (formerly LST-2, OATP8) | Liver, placenta | BL (hepatocytes) | Chemotherapy: atrasentan, hydroxyurea, methotrexate, microcystin-LR, carboplatin, cisplatin, oxaliplatin, SN-38, docetaxel, paclitaxel, imatinib, sorafenib- β-D-glucuronide |
| Other: xenobiotics: fexofenadine, deltorphin, ouabain, digoxin, rosuvastatin, valsartan, pitavastatin, BSP, rifampin, repaglinide, telmisartan, olmesartan, enalapril, DPDPE; endogenous: bilirubin conjugates, DHEAS, T3, T4, E2G, E3S, GCA, TCA, CCK-8 | ||||
| SLCO2B1 (formerly SLC21A9) | OATP2B1 (formerly OATP-B) | Widely expressed: liver, brain (blood-brain barrier), eye, small intestine, heart, kidney, lung, ovary, pancreas, placenta, skeletal muscle, spleen, testis | BL (hepatocytes, ciliary body epithelium); AP (intestine) | Chemotherapy: erlotinib, SN-38Other: xenobiotics: benzylpenicillin, bosentan, BSP, ezetimibe, fexofenadine, glibenclamide, glyburide, montelukast, statins, sulfasalazine, telmisartan; endogenous: E3S, DHEAS, TCA |
AP, apical; Bamet-R2, cis-diamminechloro-cholylglycinate-platinum(II); Bamet-UD2, cis-diammine-bisursodeoxycholate-platinum(II); BL, basolateral; BSP, bromosulfophthalein; CCK-8, cholecystokinin octapeptide; DPDPE, [D-penicillamine2,5] encephalin; E2G, estradiol-17β-glucuronide; GCA, glycocholate; MRI, magnetic resonance imaging; PGE2, prostaglandin E2; T3, triiodothyronine; T4, thyroxine; TCA; taurocholate.