Target intelligence / Profile preview

Gq protein-coupled pathway (Gq pathway)

Target
Gq pathway
Molecular classification
Signal transduction pathway, G protein-coupled receptor pathway
01

Overview

The Gq protein-coupled pathway is a major intracellular signaling cascade activated by specific G protein-coupled receptors (GPCRs) expressed on the surface of pancreatic islet cells, particularly β cells. This pathway plays a crucial role in regulating hormone secretion, especially insulin, and thus contributes to glucose homeostasis. Key receptors include muscarinic acetylcholine receptor M3, FFAR1/GPR40, and P2Y receptors. Activation leads to PLCβ activation, IP3 and DAG production, increased intracellular calcium, PKC activation, and ultimately enhanced insulin secretion. Dysregulation can contribute to impaired glucose homeostasis and diabetes mellitus development.

Other names
Gq/11 signaling pathwayPLCβ pathway in pancreatic isletsMuscarinic acetylcholine receptor M3 signaling pathwayFFAR1/GPR40 signaling pathwayP2Y receptor signaling pathway
02

Mechanism of action

Activation of phospholipase C beta (PLCβ), leading to the generation of inositol trisphosphate (IP3) and diacylglycerol (DAG). IP3 mobilizes calcium from intracellular stores, increasing cytosolic Ca²⁺ concentration. DAG activates protein kinase C (PKC). Elevated Ca²⁺ and PKC activity promote exocytosis of insulin-containing granules from β cells.

03

Biological functions

Signal transductionRegulation of insulin secretionCalcium mobilizationPKC activationExocytosis
04

Disease associations

Diabetes mellitusImpaired glucose homeostasis
05

Safety considerations

Specificity of targeting within different tissues expressing Gq-coupled receptorsPotential for off-target effects due to widespread expression of signaling components
06

Interacting drugs

Acetylcholine

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