Progress in the ligands and their complex structures of farnesoid X receptor.
- Author:
Wei-Hu LI
1
;
Jing FU
;
Ming-Yue ZHENG
;
Gui-Xia LIU
;
Yun TANG
Author Information
1. School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Anticholesteremic Agents;
chemical synthesis;
chemistry;
pharmacology;
Azepines;
chemical synthesis;
chemistry;
pharmacology;
Benzene Derivatives;
chemical synthesis;
chemistry;
pharmacology;
Chenodeoxycholic Acid;
analogs & derivatives;
chemical synthesis;
chemistry;
pharmacology;
Crystallization;
Humans;
Indoles;
chemical synthesis;
chemistry;
pharmacology;
Isoxazoles;
chemical synthesis;
chemistry;
pharmacology;
Ligands;
Molecular Structure;
Multienzyme Complexes;
chemical synthesis;
chemistry;
pharmacology;
Pregnenediones;
chemical synthesis;
chemistry;
pharmacology;
Receptors, Cytoplasmic and Nuclear;
agonists;
antagonists & inhibitors;
metabolism;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(6):704-715
- CountryChina
- Language:Chinese
-
Abstract:
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.
