2017
Journal Article
Title

Nonacidic Farnesoid X Receptor Modulators

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.
Author(s)
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.
Journal
Funder
Open Access
DOI
Additional link
Language
English