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Chapter 6

Ligand Regulation of GPCR Quaternary Structure

G protein-coupled receptors (GPCRs) have been shown not only to be activated by physiologically circulating ligands, but also by a wide variety of other molecules with pharmacological properties which act to selectively stabilize specific sets of receptor conformations that consequently regulate GPCR-modulated signalling cascades in a specific manner. In recent years, the concept of GPCR oligomerization and the ability of these receptors to form larger protein signalling complexes has become an area of intense investigation. Such processes can modulate many steps in the life of a GPCR including intracellular trafficking, folding, internalization and pharmacological properties. Oligomer formation and regulation offers novel opportunities for drug discovery and some ligands have been shown to greatly influence the formation or dissociation of pre-formed oligomers. This chapter provides both an overview of the most recent studies reporting effects of ligands on the formation or stability of GPCR oligomers, and information on the most useful strategies that have been developed to study intermolecular interactions between GPCRs.

Print publication date: 30 Aug 2011
Copyright year: 2011
Print ISBN: 978-1-84973-183-6
PDF eISBN: 978-1-84973-344-1
Citation:
From the book series:
RSC Drug Discovery