Background: Sodium Taurocholate Co-transporting Polypeptide (NTCP) and Bile Salt Export Pump
(BSEP) play significant roles as membrane transporters because of their presence in the enterohepatic circulation of
bile salts. They have emerged as promising drug targets in related liver disease.
Methods: We reviewed the literature published over the last 20 years with a focus on NTCP and BSEP.
Results: This review summarizes the current perception about structure, function, genetic variation, and regulation of
NTCP and BSEP, highlights the effects of their defects in some hepatic disorders, and discusses the application prospect
of new transcriptional activators in liver diseases.
Conclusion: NTCP and BSEP are important proteins for transportation and homeostasis maintenance of bile acids.
Further research is needed to develop new models for determining the structure-function relationship of bile acid
transporters and screening for substrates and inhibitors, as well as to gain more information about the regulatory
genetic mechanisms involved in the processes of liver injury.