Effect of Membrane Cholesterol on BSEP/Bsep Activity: Species Specificity Studies for Substrates and Inhibitors

• Published in: Drug metabolism and disposition Vol. 37; no. 9; pp. 1878 - 1886
• Main Authors: KIS, Emese, LOJA, Eniko, NAGY, Tunde, SZENTE, Lajos, HEREDI-SZABO, Krisztina, KRAJCSI, Péter
• Format: Journal Article
• Language: English
• Published: Bethesda, MD American Society for Pharmacology and Experimental Therapeutics 01.09.2009
• Subjects: Animals; ATP Binding Cassette Subfamily B Member 11; ATP-Binding Cassette Transporters - antagonists & inhibitors; ATP-Binding Cassette Transporters - metabolism; Bile Acids and Salts - metabolism; Biological and medical sciences; Biological Transport, Active; Blotting, Western; Cell Line; Cell Membrane - metabolism; Cholesterol - pharmacology; Chromans - metabolism; Cyclosporine - metabolism; Electrophoresis, Polyacrylamide Gel; Glyburide - metabolism; Humans; Hypoglycemic Agents - metabolism; Immunosuppressive Agents - metabolism; Insecta - metabolism; Kinetics; Medical sciences; Mice; Pharmacology. Drug treatments; Rats; Species Specificity; Substrate Specificity; Thiazolidinediones - metabolism; Vesicular Transport Proteins - metabolism; Substrate; Lipids; Inhibitor; Species specificity; Biological activity; Cholesterol

The efflux transporter responsible for the canalicular elimination of bile salts from the hepatocytes is the bile salt export pump (BSEP, ABCB11). Absence or inhibition of this transporter leads to bile salt retention in the hepatocyte and in turn can lead to cholestatic liver disease. We expressed...