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Nonacidic Farnesoid X Receptor Modulators

Flesch, Daniel and Cheung, Sun-Yee and Schmidt, Jurema and Gabler, Matthias and Heitel, Pascal and Kramer, Jan and Kaiser, Astrid and Hartmann, Markus and Lindner, Mara and Lüddens-Dämgen, Kerstin and Heering, Jan and Lamers, Christina and Lüddens, Hartmut and Wurglics, Mario and Proschak, Ewgenij and Schubert-Zsilavecz, Manfred and Merk, Daniel. (2017) Nonacidic Farnesoid X Receptor Modulators. Journal of Medicinal Chemistry, 60 (16). pp. 7199-7205.

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Official URL: https://edoc.unibas.ch/70164/

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Abstract

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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molecular Pharmacy (Ricklin)
UniBasel Contributors:Lamers, Christina
Item Type:Article, refereed
Article Subtype:Research Article
ISSN:1520-4804
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:16 Apr 2019 15:36
Deposited On:16 Apr 2019 15:36

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