Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 14, Issue 19, Pages 2129-2142Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026614666141112094058
Keywords
Bile acid homeostasis; Farnesoid X receptor; Natural ligands; Nuclear receptors; Synthetic ligands
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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.
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