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(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...
Autores principales: | Stefela, Alzbeta, Kaspar, Miroslav, Drastik, Martin, Kronenberger, Thales, Micuda, Stanislav, Dracinsky, Martin, Klepetarova, Blanka, Kudova, Eva, Pavek, Petr |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8414367/ https://www.ncbi.nlm.nih.gov/pubmed/34483922 http://dx.doi.org/10.3389/fphar.2021.713149 |
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