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Updated: Apr 28, 2026

Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor
Published on: January 4, 2016
Probing the Binding Site of Bile Acids in TGR5
Antonio Macchiarulo1, Antimo Gioiello1, Charles Thomas2
1Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia , 06123 Perugia, Italy.
Abstract:
TGR5 is a G-protein-coupled receptor (GPCR) mediating cellular responses to bile acids (BAs). Although some efforts have been devoted to generate homology models of TGR5 and draw structure-activity relationships of BAs, none of these studies has hitherto described how BAs bind to TGR5. Here, we present an integrated computational, chemical, and biological approach that has been instrumental to determine the binding mode of BAs to TGR5. As a result, key residues have been identified that are involved in mediating the binding of BAs to the receptor. Collectively, these results provide new hints to design potent and selective TGR5 agonists.
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