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Organic anion transporting polypeptide 2B1 (OATP2B1, encoded by SLCO2B1), OATP1B1 (SLCO1B1), and OATP1B3 (SLCO1B3) are members of the solute carrier (SLC) superfamily of membrane transporters that facilitate the uptake of a wide range of endogenous and exogenous organic anions, including drugs, toxins, bile acids, and hormones, across the plasma membrane[1][2][3][4][5]. OATP2B1 is widely expressed, including in the intestine, liver, placenta, and various endothelial tissues, and plays a key role in drug absorption, disposition, and hormone regulation[1][3]. OATP1B1 and OATP1B3 are primarily liver-specific, located on the basolateral (sinusoidal) membrane of hepatocytes, serving as gatekeepers for hepatic drug uptake and subsequent metabolism or excretion[4][6][7]. These transporters exhibit broad substrate overlap but can differ in specificity and tissue distribution. They are clinically important due to their involvement in drug–drug interactions, genetic polymorphism-related variability in drug response, and as determinants of drug-induced toxicities, particularly with statins and chemotherapeutics[1][2][3][7]. Each transporter (OATP2B1, OATP1B1, OATP1B3) should be recorded as an individual target for structured databases. "OATP2B1/1B1/1B3 transporters" is an aggregate term and should not be used as a canonical entry.
Substrate uptake via Na⁺-independent, facilitated diffusion Drug–drug interaction (inhibition or competition can alter drug absorption and clearance)
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