Protein: Solute carrier organic anion transporter family member 1B1 (SLCO1B1) (Liver-specific organic anion transporter 1) (LST-1) (OATP-C) (Organic anion transporter SLC21A6) (Sodium-independent organic anion-transporting polypeptide 2) (OATP-2) (Solute carrier family 21 member 6) (Q9Y6L6)
Organism: Homo sapiens (Human)
Function: Mediates the Na(+)-independent uptake of organic anions. Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine). Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop. Involved in the clearance of endogenous and exogenous substrates from the liver. Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition. May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs. May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate. May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver. Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment. Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions.
Subcellular location: Basolateral cell membrane {ECO:0000269|PubMed:12196548}; Multi-pass membrane protein {ECO:0000269|PubMed:12196548}. Basal cell membrane {ECO:0000269|PubMed:35307651}; Multi-pass membrane protein {ECO:0000305}. Note=Detected in basolateral membranes of hepatocytes (PubMed:12196548). Localized to the basal membrane of Sertoli cells (PubMed:35307651). {ECO:0000269|PubMed:12196548, ECO:0000269|PubMed:35307651}.
Interaction partners:
- Solute carrier family 22 member 7
- Cytochrome P450 2C8
- Cytochrome P450 3A4)
- UDP-glucuronosyltransferase 1A1
- Cytochrome P450 2C9
- Broad substrate specificity ATP-binding cassette transporter ABCG2
- Hepatic sodium/bile acid cotransporter
- ATP-dependent translocase ABCB1
- Bile salt export pump
- Cytochrome P450 2D6
Sequence:
MDQNQHLNKTAEAQPSENKKTRYCNGLKMFLAALSLSFIAKTLGAIIMKSSIIHIERRFEISSSLVGFIDGSFEIGNLLVIVFVSYFGSKLHRPKLIGIGCFIMGIGGVLTALPHFFMGYYRYSKETNINSSENSTSTLSTCLINQILSLNRASPEIVGKGCLKESGSYMWIYVFMGNMLRGIGETPIVPLGLSYIDDFAKEGHSSLYLGILNAIAMIGPIIGFTLGSLFSKMYVDIGYVDLSTIRITPTDSRWVGAWWLNFLVSGLFSIISSIPFFFLPQTPNKPQKERKASLSLHVLETNDEKDQTANLTNQGKNITKNVTGFFQSFKSILTNPLYVMFVLLTLLQVSSYIGAFTYVFKYVEQQYGQPSSKANILLGVITIPIFASGMFLGGYIIKKFKLNTVGIAKFSCFTAVMSLSFYLLYFFILCENKSVAGLTMTYDGNNPVTSHRDVPLSYCNSDCNCDESQWEPVCGNNGITYISPCLAGCKSSSGNKKPIVFYNCSCLEVTGLQNRNYSAHLGECPRDDACTRKFYFFVAIQVLNLFFSALGGTSHVMLIVKIVQPELKSLALGFHSMVIRALGGILAPIYFGALIDTTCIKWSTNNCGTRGSCRTYNSTSFSRVYLGLSSMLRVSSLVLYIILIYAMKKKYQEKDINASENGSVMDEANLESLNKNKHFVPSAGADSETHC