GPCRs Regulate Adenylyl Cylase Activity | Cell Bio | Video Textbooks - Preview

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When GPCRs bind ligands such as glucagon or epinephrine , the stimulatory G proteins get activated and, in turn, activate the membrane-bound enzyme adenylyl cyclase.
The activated enzyme converts ATP to a second messenger cyclic AMP that uses downstream kinases such as protein kinase A or PKA to regulate the metabolism of fats and sugars.
Prolonged exposure to a high concentration of ligands induces GPCR phosphorylation by PKA.