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Nonacidic Farnesoid X Receptor Modulators

 
: Flesch, D.; Cheung, S.Y.; Schmidt, J.; Gabler, M.; Heitel, P.; Kramer, J.; Kaiser, A.; Hartmann, M.; Lindner, M.; Lüddens-Dämgen, K.; Heering, J.; Lamers, C.; Lüddens, H.; Wurglics, M.; Proschak, E.; Schubert-Zsilavecz, M.; Merk, D.

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Journal of medicinal chemistry 60 (2017), No.16, pp.7199-7205
ISSN: 0022-2623
ISSN: 1520-4804
Deutsche Forschungsgemeinschaft DFG
PR 1405/2-2, PR 1405/4-1, SFB 1039
English
Journal Article
Fraunhofer IME ()

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.

: http://publica.fraunhofer.de/documents/N-480520.html