Beyond bile acids: targeting Farnesoid X Receptor (FXR) with natural and synthetic ligands.
The modulation of FXR receptor remains an attractive area in drug discovery to develop novel therapeutic opportunities for liver and metabolic disorders. Despite the large variety of FXR ligands reported so far, only a very restricted number of agonists have entered in clinical settings. In this review article we provide the reader with an overview on the different classes of natural and synthetic ligands that have been developed by academic groups and pharmaceutical companies to target FXR. We discuss their structure-activity relationships, analyzing the binding modes that some of these compounds adopt to interact with the receptor.
Andrea
A
Carotti
Maura
M
Marinozzi
Chiara
C
Custodi
Bruno
B
Cerra
Roberto
R
Pellicciari
Antimo
A
Gioiello
Dipartimento di Scienze Farmaceutiche, Via del Liceo 1 06123 Perugia, Italy. antonio.macchiarulo@unipg.it.
Antonio
A
Macchiarulo
D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism*; D006801:Humans; D008958:Models, Molecular; D011485:Protein Binding; D018160:Receptors, Cytoplasmic and Nuclear / Q000737:chemistry* / Q000378:metabolism*; D000099150:Receptor, Farnesoid X-Activated
D001647:Bile Acids and Salts; D018160:Receptors, Cytoplasmic and Nuclear; D000099150:Receptor, Farnesoid X-Activated