Farnesoid-X Receptor (FXR) as a Promising Pharmaceutical Target in Atherosclerosis

作者：Moris Demetrios; Giaginis Constantinos^*; Tsourouflis Gerasimos; Theocharis Stamatios

来源：Current Medicinal Chemistry, 2017, 24(11): 1147-1157.

DOI：10.2174/0929867324666170124151940

• FXR
• atherosclerosis
• agonist
• bile acids
• pharmaceutical target
• clinical trials

Background: Atherosclerosis (AS) is a major cause of death and morbidity in Western world and is strongly connected with atherogenic lipoproteins and inflammation. Bile acids (BA) act as activating signals of endogenous ligands such as Farnesoid-X receptor (FXR). Primary data indicate a potential role of FXR in AS. The therapeutic value of FXR ligands in AS is unknown.
Objective: With the present review, we analyzed the efficacy of FXR agonists as a therapeutic modalities against AS. In this aspect, we performed an electronic search through PubMed/MEDLINE database by using the key terms: FXR*, Farnesoid X receptor*, atherosclerosis*, bile acids* and agonism*.
Conclusion: According to our analysis, the FXR seems to be a promising therapeutic target in the atherosclerosis natural history. FXR agonism could exert protective effects in the development and evolution of AS. However, concomitant side effects such as the reduction of plasma HDL have been reported. Finally, results from undergoing clinical trials with synthetic FXR agonists will shed more light to the precise role of FXR agonism in AS treatment.

• 出版日期2017