Organic anion transporting polypeptide family (OATP family) (OATP)

The Organic Anion Transporting Polypeptide (OATP) family consists of membrane-bound influx transporters encoded by the SLCO gene superfamily that facilitate the sodium-independent uptake of diverse amphipathic organic compounds (Source: UniProt). These transporters are expressed across various tissues, with OATP1B1, OATP1B3, and OATP2B1 being particularly prominent in the liver, where they mediate the clearance of endogenous substances like bile acids, bilirubin, and thyroid hormones (Source: StatPearls). OATPs are critical determinants of the pharmacokinetics of many drugs, most notably HMG-CoA reductase inhibitors (statins), where genetic variations or drug-mediated inhibition can lead to elevated plasma levels and increased risk of adverse effects like myopathy (Source: PubMed, PMID: 23588310). In oncology, several OATP members are found to be overexpressed in solid tumors, including breast and prostate cancers, making them potential targets for targeted therapy or diagnostic imaging (Source: PubMed, PMID: 28214520). Because they handle a broad spectrum of substrates, they are a primary focus of regulatory agencies for evaluating potential drug-drug interactions during drug development (Source: FDA). They are currently recognized as key players in the disposition of approximately 50% of the top 100 prescribed drugs.

Other names

Solute carrier organic anion transporter familySLCO familyOrganic anion transportersOATPs

OATPs act as uptake transporters that facilitate the movement of organic anions across the plasma membrane into the cytoplasm, typically utilizing a counter-ion exchange mechanism involving bicarbonate, glutathione, or other intracellular anions (Source: PubMed, PMID: 21311539).