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Target intelligence / Profile preview
G-protein Coupled Bile Acid Receptor TGR5 (TGR5)
- Target
- TGR5
- Molecular classification
- G protein-coupled receptor (GPCR)
01
Overview
TGR5 is a G protein-coupled receptor that acts as a cell-surface sensor for bile acids, eliciting second messenger signaling cascades. Activation leads to increased intracellular cAMP via adenylyl cyclase activation. Key roles include regulation of energy homeostasis, induction of glucagon-like peptide‑1 (GLP‑1) secretion, modulation of inflammation, and cytoprotective properties during cholestasis. It is a potential target for treatment of metabolic diseases, cholestatic liver diseases, and portal hypertension.
- Other names
- GPBAR1G-protein coupled bile acid receptor 1GPR131M-BARGPCR19Membrane bile acid receptor
02
Mechanism of action
Gs protein activation leading to increased intracellular cAMP via adenylyl cyclase activation and triggering downstream pathways including MAP kinase signaling.
03
Biological functions
Signal transductionRegulation of energy homeostasisRegulation of metabolic rateRegulation of glucose homeostasisModulation of inflammationSmooth muscle relaxation
04
Disease associations
Metabolic diseasesType II diabetesMetabolic syndromeCholestatic liver diseasesPortal hypertension
05
Safety considerations
Possible impact on gallbladder motility/filling
06
Interacting drugs
Lithocholic acid (LCA)
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