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Let’s Go Rafting: Ligand Functional Selectivity May Depend on Membrane Structure

Department of Integrative Medical Sciences, NEOUCOM, Rootstown, OH 44272-0095

SUMMARY

Ligand functional selectivity occurs when full agonists at a single type of G protein–coupled receptor differ in their abilities to activate intracellular signaling pathways. Membrane rafts are cholesterol and sphingolipid-enriched areas of the cell membrane that tether signal protein complexes. Recent data suggests that functional selectivity of signaling through the µ opiate receptor depends on location of receptor and G proteins in raft or nonraft membrane domains. Changes in the distribution of signaling molecules in different membrane domains with age, disease, or drug history may contribute to variations in signaling and drug effects. Other results suggest that functional selectivity may account for therapeutic advantages of certain beta blockers used to treat heart failure. Functional selectivity could be exploited to develop drugs with more therapeutic value and fewer side effects.

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