Advances in farnesoid X receptor antagonists and their pharmacological activities
10.12092/j.issn.1009-2501.2020.07.008
- VernacularTitle: 法尼醇X受体拮抗剂及药理活性研究进展
- Author:
Weiyi LIU
1
Author Information
1. Key Laboratory of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University
- Publication Type:Journal Article
- Keywords:
Antagonist;
Farnesoid X receptor;
Pharmacological activity
- From:
Chinese Journal of Clinical Pharmacology and Therapeutics
2020;25(7):764-774
- CountryChina
- Language:Chinese
-
Abstract:
Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily. It has extensive physiological functions in maintaining homeostasis of bile acids, lipids, and glucose. It also participates in the development of various tumors. Therefore, regulation of its transcriptional activity is accepted as an important strategy for treatment of many diseases, and various FXR agonists have been developed. In recent years, it has been found that inhibition of FXR transcriptional activity also shows beneficial effects on various diseases, therefore several FXR antagonists have been developed and their pharmacological activities have been tested in preclinical animal models. This article provides an update review on FXR antagonists and their pharmacological activities.
