Solute carrier organic anion transporters, also known as organic-anion-transporting polypeptides (OATPs) encoded by the SLCO genes, constitute an important transporter superfamily that mediates transmembrane transport of various endo- and xenobiotics (bile acids, bilirubin, steroid hormone conjugates, thyroid hormones, prostaglandins, clinically used drugs, and toxins). Twelve human OATPs with different transport functions are expressed in various tissues. The expression of some members shows a restricted pattern (OATP1B1/OATP1B3 in the liver, OATP4C1 in the kidney, and OATP6A1 in testis). Structurally, they are 12-transmembrane glycoproteins and contain many conserved structural features that are important for substrate transport. The most well-characterized human OATPs are OATP1A2, OATP1B1, OATP1B3, and OATP2B1. Very little is known about the function and characteristics of OATP5A1 and OATP6A1. Moreover, some OATPs, such as PATP1B3, are up-regulated in malignant tissues (colon, breast, prostate). Thus, they can act as biomarkers for many tumors and can be considered as important therapeutic targets in anti-cancer drug design.
Here, we give an introduction to the following human OATPs, summarizing our knowledge about OATP transport mechanisms, functions, protein structure, and pharmacology.
|Human Solute Carrier Organic Anion Transporter Family Members|
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