Advances in understanding the regulatory mechanism of organic solute transporter α-β

The organic solute transporter α-β (OSTα-OSTβ) is a heteromeric transporter localized to the basolateral membranes of liver, intestinal, and kidney epithelial cells and functions to extrude bile acids and steroids from these tissues. OSTα-OSTβ expression is variable among species and tissues. This transporter plays important roles in maintaining BA homeostasis and may correlate with the progression of diseases relevant to cholestasis or BA malabsorption. Crosstalk between multiple nuclear receptors and cytokines reveals a more intricate means of regulating OSTα-OSTβ. Human OSTα/β and mouse Ostα/β promoters are endowed with binding sites for several transcription factors. This review aims to uncover the current regulatory mechanism of OSTα-OSTβ, explain the rationale underlying this approach and provide practical evidence. Therapeutic strategies targeting OSTα-OSTβ or its upstream regulators may be essential to correct abnormal BA levels and intervene in the progression of diseases relevant to the disturbance of BA homeostasis.