Atomic, structural and molecular insights into GPCR ligand binding and signalling.

Atomic, structural, and molecular insights reveal how GPCRs translate extracellular cues into intracellular signals, advancing understanding of their complex signalling mechanisms.

• Why it matters: GPCRs are the largest family of human membrane proteins and the primary targets of many therapeutics, yet their signalling complexity and regulation remain incompletely understood, limiting drug development.
• What they did: The review synthesizes recent advances in GPCR structure, function, and regulation at atomic, structural, and molecular levels, emphasizing ligand recognition, conformational changes, and interactions with adaptors and pathways.
• The result: This comprehensive understanding of GPCR signalling mechanisms may enable the rational design of more specific, effective, and safer medicines targeting these receptors.