Article

Engineering GPCR signaling pathways with RASSLs

Department of Medicine, University of California, San Francisco, San Francisco, California, United States
Nature Methods (Impact Factor: 25.95). 09/2008; 5(8):673-8. DOI: 10.1038/nmeth.1232
Source: PubMed

ABSTRACT We are creating families of designer G protein-coupled receptors (GPCRs) to allow for precise spatiotemporal control of GPCR signaling in vivo. These engineered GPCRs, called receptors activated solely by synthetic ligands (RASSLs), are unresponsive to endogenous ligands but can be activated by nanomolar concentrations of pharmacologically inert, drug-like small molecules. Currently, RASSLs exist for the three major GPCR signaling pathways (G(s), G(i) and G(q)). We review these advances here to facilitate the use of these powerful and diverse tools.

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    • "ective Intrabodies Regulate b 2 AR Function or global antagonist treatments can have a variety of off - target effects which make data interpretation problematic , although considerable advances have recently been made using receptor activated solely by a synthetic ligand and designer receptor exclusively activated by designer drugs technologies ( Conklin et al . , 2008 ) . In this context , intrabody expression driven by cell type – specific promoters may provide a novel strategy to examine the contribution of particular receptors and signaling pathways to regulating numerous physiological and patholog - ical processes . Additionally , the discovery of intrabodies that bias signaling may also be usefu"
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