Tryptophan Residue Located at the Middle of Putative Transmembrane Domain 11 Is Critical for the Function of Organic Anion Transporting Polypeptide 2B1

摘要: Organic anion transporting polypeptide 2B1 (OATP2B1), which is highly expressed in enterocytes and hepatocytes could be a key determinant for the intestinal absorption hepatic uptake of its substrates, most are amphipathic organic anions. Tryptophan residues may possess multitude functions transport protein through aromatic interactions, such as maintaining proper structure, guiding depth membrane insertion, or interacting directly with substrates. There totally six tryptophan OATP2B1. However, little known about their role function expression Our results show that, while W272, W276, W277 located at border extracellular loop 3 transmembrane domain 6 exhibit moderate effect on surface OATP2B1, W611 middle 11 plays critical The tryptophan-to-alanine mutation changes kinetic characteristics OATP2B1-medi...