ATP-binding cassette (ABC) transporters are an evolutionarily conserved family of proteins that catalyze the transport of molecules across extra- and intracellular membranes through the energy of ATP hydrolysis. ABC genes comprise seven subfamilies, designated ABC1, Mdr/TAP, MRP, ALD, OABP, GCN20 and White. The secretion of bile salt molecules from blood into bile is a major driving force for bile formation. Bile salt export pump (BSEP) is a member of the Mdr/TAP subfamily of ABC transporters that mediates the transport of bile acids across the hepatocyte canalicular membrane and regulates bile acid-dependent bile secretion. BSEP contains putative phosphorylation sites for protein kinase A, protein kinase C (PKC) and Ca2+-calmodulin dependent kinase II, whose regulation may be dependent on bile salt concentration.