5 years ago

Nonacidic Farnesoid X Receptor Modulators

Nonacidic Farnesoid X Receptor Modulators
Jurema Schmidt, Mara Lindner, Daniel Flesch, Ewgenij Proschak, Kerstin Lüddens-Dämgen, Christina Lamers, Jan Heering, Jan Kramer, Manfred Schubert-Zsilavecz, Pascal Heitel, Matthias Gabler, Markus Hartmann, Hartmut Lüddens, Daniel Merk, Mario Wurglics, Astrid Kaiser, Sun-Yee Cheung
As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. Clinical results have validated FXR as therapeutic target in hepatic and metabolic diseases. To date, potent FXR agonists share a negatively ionizable function that might compromise their pharmacokinetic distribution and behavior. Here we report the development and characterization of a high-affinity FXR modulator not comprising an acidic residue.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00903

DOI: 10.1021/acs.jmedchem.7b00903

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