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

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 19 , 2014

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Graphical 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.

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

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Article Details

Year: 2014
Page: [2175 - 2187]
Pages: 13
DOI: 10.2174/1568026614666141112101840
Price: $65

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