Abstract
Publisher Summary The diversity of G protein-coupled receptors (GPCRs) presents a challenge to understanding the connection between a single receptor signaling pathway and a specific physiological or pathological response. Receptors activated solely by synthetic ligands (RASSLs) offer control over the location, timing, and specificity of a G protein signal in vivo. These novel, reversible switches for G protein signaling have clarified the role of Gi signaling in cardiac physiology and are now being used to probe sensory transduction and complex neurobehavioral responses. This chapter summarizes the design of RASSLs and their first use in vivo. Existing RASSLs will allow study of the effects of Gi signaling in specific tissues under specific circumstances. New RASSLs can be developed by using many of the same principles used to develop the existing Gi-coupled RASSLs. The ideal RASSL activator should be a small molecule drug that is readily available from commercial sources. Its binding site should be well characterized. It must be highly specific for a single receptor subtype to minimize effects of the drug at non-RASSL receptors. Ideally, this could be a synthetic system in which the ligand would not activate endogenous receptors.
Published Version
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