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Domain

A conserved histidine residue in the third TMD (His-115) may play an essential role in the pH sensitivity of SLCO1B3/OATP1B3-mediated substrate transport.

Function

Mediates the Na(+)-independent uptake of organic anions (PubMed:10779507, PubMed:15159445, PubMed:17412826). Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) (PubMed:10779507, PubMed:11159893, PubMed:12568656, PubMed:15159445, PubMed:17412826, PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate 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 (PubMed:19129463). Involved in the clearance of bile acids and organic anions from the liver (PubMed:22232210). Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop (PubMed:22232210). Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition (PubMed:26383540). 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 pitavastatin, a clinically important class of hypolipidemic drugs (PubMed:15159445). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). 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 (PubMed:16624871, PubMed:16627748).

Involvement in disease

Hyperbilirubinemia, Rotor type

HBLRR

An autosomal recessive form of primary conjugated hyperbilirubinemia. Affected individuals develop mild jaundice not associated with hemolysis shortly after birth or in childhood. They have delayed plasma clearance of the unconjugated anionic dye bromsulphthalein and prominent urinary excretion of coproporphyrin I. Hepatic pigmentation is normal.

None

The disease is caused by variants affecting the gene represented in this entry.

Post-translational modifications

N-glycosylated.

Sequence similarities

Belongs to the organo anion transporter (TC 2.A.60) family.

Tissue specificity

Highly expressed in liver, in particular at the basolateral membrane of hepatocytes near the central vein (PubMed:10779507, PubMed:15159445). Expressed in the placenta (PubMed:12409283). In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and within the tubules (PubMed:35307651).

Cellular localization

  • Basolateral cell membrane
  • Multi-pass membrane protein
  • Basal cell membrane
  • Multi-pass membrane protein
  • Localized to the basolateral membrane of hepatocytes (PubMed:10779507). Localized to the basal membrane of Sertoli cells (PubMed:35307651).

Alternative names

LST2, OATP1B3, OATP8, SLC21A8, SLCO1B3, Solute carrier organic anion transporter family member 1B3, Liver-specific organic anion transporter 2, Organic anion transporter 8, Organic anion-transporting polypeptide 8, Solute carrier family 21 member 8, LST-2, OATP-8

Target type

Proteins

Primary research area

Metabolism

Molecular weight

77403Da

We found 5 products in 1 category

Primary Antibodies

Application

Reactive species