Perspective abstract
Nature Chemical Biology 4, 397 - 403 (2008)
Published online: 17 July 2008 | doi:10.1038/nchembio.97
Insights into signaling from the 
2-adrenergic receptor structure
Martin Audet1 & Michel Bouvier1
Abstract
With more than 800 members, the G protein–coupled receptor family constitutes the largest group of membrane proteins involved in signal transduction. Until the end of last year, high-resolution three-dimensional structures were available for only one of them—the light receptor rhodopsin. Recently the structure of the 
2-adrenergic receptor has been obtained, and it revealed interesting differences with the structure of rhodopsin. Analyses of these differences raise important questions about the binding modes of diffusible ligands in the receptor and allow formulation of testable hypotheses about the structural determinants linking drug binding to specific signaling responses. The three-dimensional structure derived from the 2-adrenergic receptor crystal has been used to virtually dock ligands with distinct activities. The different binding modes of these ligands, which correlated with their reported efficacy profiles, suggest that it could be possible to predict the structural determinants of drug signaling efficacies.
- Martin Audet and Michel Bouvier are in the Department of Biochemistry, Institute for Research in Immunology and Cancer, and Groupe de Recherche Universitaire sur le Médicament, Université de Montréal, C.P. 6128 Succursale Centre-Ville, Montréal, Québec H3C 3J7, Canada. e-mail: michel.bouvier@umontreal.ca
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