Farnesoid X receptor (FXR) belongs to the nuclear receptor superfamily.  It is highly related to the formation of metabolic syndrome and the glucose homeostasis, and therefore represents an important drug target against metabolic diseases and diabetes.  In recent years, great progress has been made in the agonists, antagonists, and crystal structures of FXR.  The diverse FXR ligands and their structure-activity relationship are reviewed in this article.  The advances in the crystal structures of FXR in complex with different ligands are also introduced.