SLCO1B1

(redirected from OATP1B1)

SLCO1B1

A gene on chromosome 12p12 that encodes a transporter which mediates Na+-independent uptake of organic anions—e.g., pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl oestradiol, oestrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. SLCO1B1 may play a key role in clearing bile acids and organic anions from the liver.

Molecular pathology
Defects in SLCO1B1 are a cause of Rotor syndrome.
References in periodicals archive ?
Co-administration of VIEKIRAX with drugs that are substrates of CYP3A4, P-gp, BCRP, OATP1B1 or OATP1B3 may result in increased plasma concentrations of such drugs, potentially requiring dose adjustment or clinical monitoring.
The transporters recommended for initial assessment generally Included those for which A clinical relevance to drug disposition has Been identified, namely, the efflux transporters P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP), and the uptake transporters OCT2, OAT1, OAT3, OATP1B1 and OATP1B3.
Fang, "The Role of OATP1B1 and BCRP in Pharmacokinetics and DDI of Novel Statins," Cardiovascular Therapeutics (2011).
OATP1B1 polymorphism is a major determinant of serum bilirubin level but not associated with rifampicin-mediated bilirubin elevation.
Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination.
Because of the structure and size of MCs, active uptake into cells occurs via organic anion-transporting polypeptides (OATP/Oatp), as confirmed for liver-specific human OATP1B1 and OATP1B3, mouse Oatp1b2 (mOatp 1b2), skate Oatp 1d1, and the more widely distributed OATP1A2 expressed, for example, at the blood--brain barrier.
OATP1B1 and 1B3 in the liver) (Hagenbuch and Meier 2004).
In vitro studies have also demonstrated that eltrombopag is an inhibitor of OATP1B1 and a variety of uridine 5'-diphospho-glucuronosyltransferases; patients receiving medications that are metabolized through any of these pathways should be monitored for excessive drug exposure.
As the role of SLCO1B1 gene (encodes OATP1B1 or liver specific transporter-1) 388 A>G polymorphism in susceptibility towards gallstone disease is unclear the prevalence of this polymorphism in healthy north Indian population was investigated.
Sigma-Aldrich plans to knock-out genes for critical xenobiotic sensors-such as PXR and CAR-and drug transporters-including BSEP, OATP1B1, and OATP1B3-that regulatory agencies have highlighted for possible analysis.
2007) reported that the expression of the human hepatocyte uptake transporter OATP1B1 or OATP1B3 was critical for the selective uptake of microcystin-LR into hepatocytes and for induction of its fatal cytotoxicity.
The seven identified transporters are: the efflux transporters P-glycoprotein (P-gp, MDR1, ABCB1) and BCRP (ABCG2); organic cation transporter OCT2 (SLC22A2); organic anion transporters OAT1 (SLC22A6) and OAT3 (SLC22A8); and organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3).