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Target intelligence / Profile preview
G-protein coupled bile acid receptor 1 (GPBAR1)
- Target
- GPBAR1
- Molecular classification
- G protein-coupled receptor
01
Overview
G-protein coupled bile acid receptor 1 (GPBAR1), also known as TGR5, is a G protein-coupled receptor that binds bile acids and mediates their signaling effects. Activation of GPBAR1 leads to increased cAMP levels, ERK activation, GLP-1 secretion, and anti-inflammatory effects. It is expressed in various tissues, including the gastrointestinal tract, liver, immune system, and nervous system. GPBAR1 is a promising target for diabetes treatment, but safety concerns regarding gallbladder toxicity need to be addressed.
- Other names
- TGR5GPCR19BG37GPR131M-BAR
02
Mechanism of action
Agonism leading to increased cAMP levels and ERK activation
03
Biological functions
Signal transductionMetabolic regulationGLP-1 secretionAnti-inflammatory effectsVasodilation regulation
04
Disease associations
DiabetesCholestatic liver injuryLiver cirrhosisInflammation
05
Safety considerations
Gallbladder toxicity with some agonists
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