Overview of organic anion transporters and organic anion transporter polypeptides and their roles in the liver

Table 1 Organizational characteristics and substrates of human organic anion transporters[4,14,21,45,63,151,152,153]

Protein name	Alias	Chromosome localization	Distribution location	Substrates (Km value)
OAT1	SLC22A6	11q13.1	Kidney, brain, liver, stomach, pancreas	P-aminohippurate (PAH; 5 μmol), prostaglandin E2 (PGE2; 0.97 μmol), α-ketoglutaric acid, captopril, methotrexate
OAT2	SLC22A7	6p21.1	Liver, kidney, embryonic liver and kidney	PAH, PGE2 (0.71 μmol), estrone-3-sulfate (E3S), α-ketoglutaric acid (17.8 μmol), cGMP, succinic acid, paclitaxel (0.14 μmol), dehydroepiandrosterone (DHEA) sulfate, methotrexate, diclofenac, acyclovir, penciclovir, theophylline (12.6 μmol), erythromycin (18.5 μmol), salicylate (88.8 μmol)
OAT3	SLC22A8	11q11.7	Kidney, brain, liver, skeletal muscle, adrenal gland	PAH (87 μmol), PGE2 (0.34 μmol), E3S (3 μmol), zidovudine, cimetidine, bumetanide, ciprofloxacin, benzylpenicillin, pravastatin, methotrexate, bile acids, amino acids, MTX (11 μmol)
OAT4	SLC22A11	11q12.3	Kidney, placenta, adrenal gland	Urate, PGE2 (0.15 μmol), E3S (1 μmol), PAH, olmesartan, methotrexate, bumetanide
OAT5	SLC22A10	11q12.3	Liver	Unknown
OAT6	SLC22A20	11q13.1	Olfactory mucosa	E3S, PAH, PGE2, ibuprofen, ochratoxin A (OTA)
OAT7	SLC22A9	11q12.3	Liver	E3S, DHEA, sulfate, butyrate
OAT8	UST6	11q12.3	Liver	Unknown
OAT9	SLC22A27	Unknown
OAT10	SLC22A13	3p22.2	Kidney, brain, heart, colon	Lactate, nicotinate, succinate, glutathione urate
URAT1	SLC22A12	11q13.1	Kidney, vascular smooth muscle cells, liver, lung	Urea, chloride
S22AO	SLC22A24	11q12.3	Kidney	Unknown
OCTL2	SLC22A14	3p22.2	Testis, kidney	Unknown

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