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Bile acid receptor pathway

Molecular classification
Nuclear hormone receptor (e.g., Farnesoid X receptor [FXR], Retinoid-related orphan receptor γt [RORγt], Vitamin D receptor [VDR], Pregnane X receptor [PXR], Constitutive androstane receptor [CAR]), G protein-coupled receptor (e.g., G protein-coupled bile acid receptor 1 [GPBAR1 or TGR5]), Other
01

Overview

Bile acids pathway modulation" is not a single molecular target but refers to the therapeutic targeting of multiple **bile-acid-sensing receptors**—primarily the **Farnesoid X Receptor** (*FXR*), **G protein-coupled bile acid receptor 1** (*TGR5/GPBAR1*), and others such as VDR, PXR, CAR—which are key regulators in metabolic processes. These nuclear and membrane-bound receptors mediate the effects of endogenous and synthetic ligands on lipid/glucose metabolism, immune responses, nutrient absorption, hepatic function, and gut microbiota composition. Pharmacological manipulation through natural or synthetic agonists/antagonists has shown efficacy in treating conditions like cholestatic liver diseases, type 2 diabetes mellitus, non-alcoholic fatty liver disease/nonalcoholic steatohepatitis (*NAFLD/NASH*), inflammatory bowel disease (*IBD*), obesity/metabolic syndrome. The field is rapidly evolving with new drugs targeting these pathways entering clinical use or trials. However, "Bile acids pathway modulation" is a broad process rather than a discrete molecule/receptor; thus it should be mapped to its constituent targets for structured data extraction purposes[1][2][3].

Other names
Bile acid signalingFXR/TGR5 pathwaybile acid receptorsbile acid metabolism modulation
02

Mechanism of action

Agonism or antagonism of nuclear and membrane-bound bile acid receptors such as FXR and TGR5[1][2]; Modulation of gene expression involved in lipid/glucose homeostasis, inflammation, fibrosis[4]; Alteration of gut microbiota composition to influence host metabolic pathways[5]

03

Biological functions

Regulation of lipid and glucose metabolismSignal transductionImmune response modulationNutrient absorption facilitationModulation of gut microbiota composition
04

Disease associations

Metabolic syndromeDiabetes mellitus (type 2)Non-alcoholic fatty liver disease (NAFLD)Cholestatic liver diseases (e.g., primary biliary cirrhosis, primary sclerosing cholangitis)Inflammatory bowel disease (IBD)Obesity
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Safety considerations

Pruritus with potent FXR agonists like obeticholic acid[1]Potential alterations in cholesterol homeostasis/lipid profiles[4]Gastrointestinal side effects due to changes in microbiome or bile flow
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Interacting drugs

Ursodeoxycholic acid (UDCA)

5 more in the full profile.

07

Biomarkers

Serum levels of specific bile acidsLiver function tests/enzymes for cholestasis monitoringHistological markers in NAFLD/NASH studies

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