Solute carrier organic anion transporter family member 1B2 (OATP1B2)

Organic anion-transporting polypeptide 1B2 (OATP1B2) is a liver-specific uptake transporter primarily found in rodents (mice and rats), serving as the functional ortholog of the human OATP1B1 and OATP1B3 transporters. It is localized to the basolateral (sinusoidal) membrane of hepatocytes, where it mediates the sodium-independent uptake of a wide range of endogenous compounds, including bile acids, bilirubin, and steroid conjugates, as well as numerous xenobiotics and drugs. OATP1B2 plays a critical role in the hepatic clearance and systemic disposition of clinically important drugs such as statins (e.g., pravastatin), antibiotics (e.g., rifampin), and chemotherapeutic agents (e.g., paclitaxel and vincristine). Beyond its role in the liver, OATP1B2 has been identified as a key mediator of drug-induced toxicities; for instance, its expression in the dorsal root ganglia (DRG) facilitates the accumulation of neurotoxic drugs like vincristine and paclitaxel, leading to peripheral neuropathy. Consequently, OATP1B2 and its human counterparts are considered therapeutic targets for pharmacological inhibition to prevent such side effects without compromising systemic drug efficacy. Additionally, OATP1B2 is a major site for drug-drug interactions, as many drugs can inhibit its function, leading to elevated plasma levels of co-administered substrates and potential toxicity.

Other names

Oatp1b2Slco1b2Slc21a10Oatp4Lst-1rlst-1mlst-1Liver-specific organic anion transporter 1

Transporter-mediated cellular uptake of substrates; pharmacological inhibition of transport function to prevent tissue-specific toxicity.