Concept:
G-Protein Coupled Receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes.
• They play a fundamental role in transmitting signals from outside the cell to the interior.
• These receptors interact with specialized proteins called G-proteins.
Step 1: The Mechanism of Activation.
GPCRs are transmembrane proteins that cross the lipid bilayer seven times.
When a ligand (like a hormone or neurotransmitter) binds to the extracellular part of the receptor, the receptor undergoes a conformational change.
Step 2: Downstream Signaling.
This change allows the internal part of the receptor to act as a Guanine nucleotide Exchange Factor (GEF).
It triggers the associated G-protein to swap its bound GDP for GTP, thereby "activating" the G-protein.
The activated G-protein then dissociates and triggers further intracellular messengers.
Final Answer:
Activation of GPCRs directly leads to G-protein activation.