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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Medicinal chemistry of farnesoid X receptor ligands: from agonists and antagonists to modulators
Daniel Merk1, Dieter Steinhilber, Manfred Schubert-Zsilavecz
1Institute of Pharmaceutical Chemistry, Goethe University, Frankfurt, Max-von-Laue-Strausse 9, D-60438 Frankfurt am Main, Germany. merk@pharmchem.uni-frankfurt.de
Abstract:
The nuclear receptor farnesoid X receptor (FXR) has emerged as a highly promising target in preclinical development in recent years. A significant amount of research has been conducted and, although none has reached clinical use, many synthetic ligands of FXR have been described. This review outlines the available knowledge regarding the medicinal chemistry and SAR of these FXR ligands, and discusses the molecular interactions of the compounds with the FXR ligand-binding domain by interpreting the existing co-crystal structures.
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