Counter-regulatory role of bile acid activated receptors in immunity and inflammation

Current Molecular Medicine
Stefano FiorucciFranco Baldelli

Abstract

In addition to their role in dietary lipid absorption bile acids are signaling modules activating nuclear receptors and at least one G-protein coupled receptors named the TGR5. With a different rank of potency primary and secondary bile acids activates a subset of nuclear receptors including the farnesoid-X-receptor (FXR, NR1H4); the constitutive androstane receptor (CAR, NR1H3), the pregnane-x- receptor (PXR, NR1H2), the vitamin D receptor (VDR, NR1H1). Originally, these receptors were characterized for their role as bile acid and xenobiotic sensors, emerging evidence, however, indicates that FXR, PXR and VDR and their ligands are important for the modulation of immune and inflammatory reactions in entero-hepatic tissues. The immune phenotype FXR deficient mice indicates that these receptors are essential for the maintenance of immune homeostasis. A common theme of all bile acid-activated receptor is their ability to counter-regulate effector activities of cells of innate immunity establishing that signals generated by these receptors and their ligands function as a braking signals for inflammation in entero-hepatic tissues. In this review, we will spotlight the molecular mechanisms of receptor/ligand function and how bile aci...Continue Reading

Citations

Aug 29, 2018·Frontiers in Immunology·Stefano FiorucciEleonora Distrutti
Apr 15, 2021·Expert Opinion on Drug Discovery·Stefano FiorucciEleonora Distrutti
Jun 3, 2021·Cells·Michele BiagioliStefano Fiorucci
Apr 19, 2019·ACS Medicinal Chemistry Letters·Valentina SepeAngela Zampella

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