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G-protein-coupled receptor signaling pathway (GPCR pathway)

Target
GPCR pathway
01

Overview

The G-protein-coupled receptor (GPCR) signaling pathway is a fundamental mechanism by which cells sense and respond to a wide variety of external signals, including hormones, neurotransmitters, odors, light, and more. GPCRs are the largest family of membrane receptors in eukaryotes and play critical roles in numerous physiological processes such as vision, taste, smell, mood regulation, immune responses, metabolism, and behavior. Dysfunction in this pathway is implicated in diseases such as diabetes mellitus type 2, obesity, depression/anxiety disorders, cancer progression/metastasis and neurodegenerative diseases like Alzheimer’s disease. Over 500 FDA-approved drugs act via these pathways making them attractive for therapeutic intervention.

02

Mechanism of action

Modulation of intracellular effectors such as adenylyl cyclase or phospholipase C via G protein activation, leading to second messenger generation and downstream kinase activation.

03

Biological functions

Signal transduction
04

Disease associations

Diabetes mellitus type 2ObesityDepression/anxiety disordersCancer progression/metastasisNeurodegenerative diseases (e.g., Alzheimer’s disease)
05

Safety considerations

GPCR dysfunction is implicated in various diseasesTherapeutic challenges related to selectivity and off-target effects
06

Interacting drugs

Dopamine

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