OATP2B1 (previously known as OATP-B) is expressed in various tissues, including the liver, intestine, placenta, heart and skin. In the liver, OATP2B1 is expressed in the sinusoidal membrane of hepatocytes, indicating the mediation of hepatic uptake of endogenous compounds like estrone−sulfate, taurocholate, leukotriene, prostaglandin, thromboxane and drugs from blood. In the intestine, OATP2B1 is expressed in the luminal membrane of small intestinal enterocytes, suggesting that it facilitate the active absorption of bile acid metabolites, nutrients and of cures oral administered drugs. In the heart, OATP2B1 is expressed in the vascular endothelium and might thus mediate the uptake of its endogenous substrate and drugs into the heart.

Main localization:
Liver, intestine, placenta
Transporter assay:
Uptake transporter assay
Probe substrates:
Estrone-3-sulfate (ES)
Probe inhibitors:
Glibenclamide, rifampicin
Regulatory relevance:
Important interacting drugs:
Statins, glibenclamide, saquinavir, bosentan, gemfibrozil, indinavir, montelukast, paclitaxel, fexofenadin, MK-571

Inhibition of hOATP2B1-mediated ES uptake by different inhibitors (100 µM)
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