Abstract: Bile acid can not only emulsify fat and facilitate the absorption of fat soluble substances, but also it is an important signaling molecules that plays an important physiological role by activating specific bile acid receptors. Takeda G protein coupled receptor 5 (TGR5) is a membrane receptor of the bile acid, it can activate Gprotein effectors and promote the expre ssion of the second messenger and activate a variety of signal transduction pathways to exert physiological functions. The obstructive jaundice bile acid can cause a series of pathophysiological reactions through activating TGR5, which plays a significant role in the obstructive jaundice. In this article, the latest researches about the function and molecular mechanism of TGR5 in obstructive jaundice were reviewed in order to provide a new idea for exploring the new method and strategy to cure the disease.