Ligand regulation of GPCR quaternary structure

Saenz del Burgo, L. and Milligan, G. (2011) Ligand regulation of GPCR quaternary structure. In: Giraldo, J. and Pin, J.-P. (eds.) G Protein-Coupled Receptors: From Structure to Function G Protein-Coupled Receptors: From Structure to Function. Series: RSC drug discovery (8). RSC Publishing: Cambridge, UK, pp. 111-152. ISBN 9781849733441 (doi: 10.1039/9781849733441-00111)

Abstract

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.

• Item Type: Book Sections
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Saenz del Burgo, Dr Laura and Milligan, Professor Graeme
• Authors: Saenz del Burgo, L., and Milligan, G.
• College/School: College of Medical Veterinary and Life Sciences > School of Molecular Biosciences; College of Medical Veterinary and Life Sciences > School of Life Sciences
• Publisher: RSC Publishing
• ISBN: 9781849733441

Project Code	Award No	Project Name	Principal Investigator	Funder's Name	Funder Ref	Lead Dept
51063	1	The organisational structure of class A GPCRs: implications for function and drug design	Graeme Milligan	Medical Research Council (MRC)	G0900050	Institute of Neuroscience and Psychology