Table 1.
Functional roles of bile acid receptors in the gut.
Section | Receptor | Major functions in the intestine | Consequences of loss of function | Selected references |
---|---|---|---|---|
Nuclear receptors | ||||
2.1 | Farnesoid X receptor (FXR) | • Bile acid and cholesterol homeostasis via ileal FGF15/19 • Suppression of mucosal immune response • Maintenance of intestinal barrier |
• Increased susceptibility to intestinal inflammation • Bacterial overgrowth • Increased bile acid production, bile acid diarrhea • Promoting colorectal tumorigenesis |
3,6,7 |
2.2 | Vitamin D receptor (VDR) | • Detoxification • Modulation of bile acid biosynthesis via FGF15/19 |
3,30 | |
2.2 | Pregnane X receptor (PXR) | • Detoxification | 3,36 | |
2.2 | Constitutive androstane receptor (CAR) | • Detoxification | 3,36 | |
Membrane receptors | ||||
3.1 | Takeda G protein-coupled receptor (TGR5; GPBAR1) | • Delayed gastric emptying • Increased colonic motility • Anti-inflammatory response • Induction of incretin secretion and modulation of glucose homeostasis via GLP-1 |
• Disturbed motility that varies between intestinal regions • Reduced frequency of defecation • Low stool water content • Disturbed glucose homeostasis? |
37,54,77 |
3.2 | Muscarinic acetylcholine receptor M3 (M3R) | • Cell proliferation | 87 | |
3.3 | Sphingosine-1-phosphate receptor 2 (S1PR2) | • Hepatic lipid homeostasis • Cell proliferation? |
90,94 |