DEFINITION
The cAMP / PKA signalling module is the canonical downstream pathway of Gαs-coupled GPCRs. Agonist binding activates adenylyl cyclase, elevating intracellular cyclic AMP, which binds the regulatory subunits of protein kinase A (PKA) and releases active catalytic subunits.
Active PKA phosphorylates a wide range of substrates — ion channels, exocytotic proteins, metabolic enzymes and transcription factors such as CREB. At GLP-1R, cAMP / PKA signalling is a principal driver of β-cell insulin secretion and gene-expression changes.
WHY IT MATTERS
cAMP / PKA is the primary intracellular signalling module engaged by GLP-1 receptor activation.
RELATED
Compounds