Recent Advances in Non-Steroidal FXR Antagonists Development for Therapeutic Applications

Title:Recent Advances in Non-Steroidal FXR Antagonists Development for Therapeutic Applications

Volume: 14 Issue: 19

Author(s): Huang Huang, Yong Xu, Jin Zhu and Jian Li

Affiliation:

Keywords: Cholestasis, Farnesoid-x-receptor, Non-steroidal antagonist, Pharmacological target.

Abstract: Farnesoid X receptor (FXR, NR1H4), a nuclear receptor (NR) highly expressed in the liver, intestine, kidney, adrenal glands and other cholesterol-rich tissues, functions as the master regulator for bile acid homeostasis. FXR, which regulates the expression of genes encoding proteins involved in cholesterol homeostasis, plays an essential role in regulating cholesterol, lipid, and glucose metabolism. Recently, some FXR agonists are reported to have low selectivity on NRs, which forces the researchers to move their eyes onto the development of FXR antagonists with high selectivity. The development of non-steroidal FXR antagonists with different scaffolds including AGN34, tuberatolides, atractylenolides, andrographolides, GW4064 derivatives and 1,3,4-trisubstitutedpyrazolones, provides us a prospect for the therapy of in ammation, metabolic syndrome, diabetes, cholesterol gallstones, and cancer.

Cite this article as:

Huang Huang, Xu Yong, Zhu Jin and Li Jian, Recent Advances in Non-Steroidal FXR Antagonists Development for Therapeutic Applications, Current Topics in Medicinal Chemistry 2014; 14 (19) . https://dx.doi.org/10.2174/1568026614666141112101840