β‐arrestins and heterotrimeric G‐proteins: collaborators and competitors in signal transduction

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Abstract
G‐protein‐coupled receptors (GPCRs), also known as seven transmembrane receptors (7‐TMRs), are the largest protein receptor superfamily in the body. These receptors and their ligands direct a diverse array of physiological responses, and hence have broad relevance to numerous diseases. As a result, they have generated considerable interest in the pharmaceutical industry as drug targets. Recently, GPCRs have been demonstrated to elicit signals through interaction with the scaffolding proteins, β‐arrestins‐1 and 2, independent of heterotrimeric G‐protein coupling. This review discusses several known G‐protein‐independent, β‐arrestin‐dependent pathways and their potential physiological and pharmacological significance. The emergence of G‐protein‐independent signalling changes the way in which GPCR signalling is evaluated, from a cell biological to a pharmaceutical perspective and raises the possibility for the development of pathway specific therapeutics.British Journal of Pharmacology(2008)153, S298–S309; doi:10.1038/sj.bjp.0707508; published online 26 November 2007