[Progress in the ligands and their complex structures of farnesoid X receptor].
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.
School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Wei-Hu
WH
Li
Jing
J
Fu
Ming-Yue
MY
Zheng
Gui-Xia
GX
Liu
Yun
Y
Tang
D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001555:Benzene Derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002635:Chenodeoxycholic Acid / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D003460:Crystallization; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D015394:Molecular Structure; D009097:Multienzyme Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011282:Pregnenediones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D000099150:Receptor, Farnesoid X-Activated
D000924:Anticholesteremic Agents; D001381:Azepines; D001555:Benzene Derivatives; D002635:Chenodeoxycholic Acid; D007211:Indoles; D007555:Isoxazoles; D008024:Ligands; D009097:Multienzyme Complexes; D011282:Pregnenediones; D018160:Receptors, Cytoplasmic and Nuclear; D000099150:Receptor, Farnesoid X-Activated; C540004:WAY-362450; C474615:fexaramine; C023617:pregna-4,17-diene-3,16-dione; C412815:GW 4064