(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

Bile acids (BAs) are key signaling steroidal molecules that regulate glucose, lipid, and energy homeostasis via interactions with the farnesoid X receptor (FXR) and G-protein bile acid receptor 1 (GPBAR1). Extensive medicinal chemistry modifications of the BA scaffold led to the discovery of potent...

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Bibliographic Details
Main Authors: Alzbeta Stefela, Miroslav Kaspar, Martin Drastik, Thales Kronenberger, Stanislav Micuda, Martin Dracinsky, Blanka Klepetarova, Eva Kudova, Petr Pavek
Format: Article
Language:English
Published: Frontiers Media S.A. 2021-08-01
Series:Frontiers in Pharmacology
Subjects:
G protein-coupled bile acid receptor 1
bile acids
steroid
farnesoid X receptor
metabolism
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2021.713149/full

Internet

https://www.frontiersin.org/articles/10.3389/fphar.2021.713149/full

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