Table 2.
Organizational characteristics and substrates of human organic anion transporter polypeptides[4,25,69,73,153,154,155,156]
| Protein name | Coding gene | Chromosome localization | Distribution location | Substrates (Km value) |
| OATP1A2 | SLCO1A2 | 12p12.1 | Brain, liver, kidney | Bile salts, bilirubin, ciprofloxacin, estrone-3-sulfate (59 μmol), methotrexate, N-methylquinidine (26 μmol), norfloxacin, PGE2, taurochenodeoxycholate (19 μmol) |
| OATP1B1 | SLCO1B1 | 12p12.1 | Liver | Benzylpenicillin, bile acid, bilirubin (8 μmol), estradiol-17b-glucuronide (8 μmol), estrone-3-sulfate (0.2 μmol), methotrexate, olmesartan, pravastatin (35 μmol), taurocholate (10-34 μmol), steroid hormone |
| OATP1B3 | SLCO1B3 | 12p12.2 | Liver | Benzylpenicillin (penicillin G), bilirubin (39 μmol), bile acid, cholecystokinin octapeptide (CCK-8; 11 μmol), docetaxel, eicosanoid, estradiol-17β-glucuronide (5.4 μmol), methotrexate (25 μmol), paclitaxel (7 μmol), rosuvastatin, saquinavir, steroid hormone, taurocholate (6 μmol) |
| OATP1C1 | SLCO1C1 | 12p12.2 | Brain, testis | Bromosulfophthalein, estrone-3-sulphate, thyroid hormones (0.1 μmol) |
| OATP2A1 | SLCO2A1 | 3q22.1-q22.2 | Brain, colon, heart, kidney, liver, small intestine, stomach | PGH2, PGE1 (82 μmol), PGE2 (100 μmol), PGF2a (92 μmol), thromboxane B2 (182 μmol) |
| OATP2B1 | SLCO2B1 | 11q13.4 | Liver, intestinal epithelium, placenta, epidermal keratin, breast, heart, skeletal muscle, brain | Benzylpenicillin, bilirubin, dehydroepiandrosterone-3-sulphate, estrone-3-sulphate (5 μmol), fexofenadine, montelukast, pravastatin, pitavastatin, PGE2, talinolol, statins, steroids, taurocholate |
| OATP3A1 | SLCO3A1 | 15q26.1 | Testis, brain, heart, lung, spleen | Benzylpenicillin, estrone-3-sulphate, PGE1, PGE2, PGF2a, steroid hormone |
| OATP4A1 | SLCO4A1 | 20q13.33 | Heart, placenta, lung, liver, skeletal muscle, kidney, pancreas | Bile salts, estrone-3-sulphate, PGE2, taurocholate (15 μmol), steroid hormone |
| OATP4C1 | SLCO4C1 | 5q21.1 | Liver | Bile salts, cAMP, digoxin (8 μmol), estrone-3-sulphate, methotrexate, steroid hormone |
| OATP5A1 | SLCO5A1 | 8q13.3 | Fetal brain, prostate, skeletal muscle | Satraplatin |
| OATP6A1 | SLCO6A1 | 5q21.1 | Testis, spleen, brain, fetal brain, placenta | Unknown |