Recent developments in GPCR signalling

Recent developments in GPCR signalling

1. Signalling pathway activated by a receptor in a cell is context specific

   • In different cells in the body or in the same cell at different times, different things are happening
   • Results in greater control over physiological outcome

2. Specific signalling is regulated by

   • Adaptor proteins
   • Scaffold proteins
     • Play an important role in bringing receptors together with certain pathways
   • Lipids (Association with rafts/lipid microdomains)
   • Endocytosis
   • Splicing
   • Post-translational modifications

3. Regulation through interacting proteins

   • RAMPS
   • GRKs
     • 7 types
   • B-arrestins
     • 4 types
   • RGS proteins

4. Therapeutic potential of agonist-biased signalling

   • Does μ-opioid receptor (MOR) desensitization and trafficking have any role in tolerance?

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