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Trends Pharmacol Sci. 2001 Aug;22(8):414-20.

Engineering receptors activated solely by synthetic ligands (RASSLs).

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Gladstone Institute of Cardiovascular Disease, Gladstone Institute of Neurological Disease, Depts of Medicine and Pharmacology, University of California, San Francisco, PO Box 419100, San Francisco, CA 94141-9100, USA.


The functional and molecular diversity of G-protein-coupled receptors presents a significant challenge to understanding the connection between a single receptor signaling pathway and a specific physiological or pathological response. To gain control over the timing and specificity of a G-protein signal, receptors activated solely by synthetic ligands (RASSLs) have been developed. These engineered receptors no longer respond to endogenous peptides, but can still be activated by a specific small-molecule drug. Further control over the location of the signal can be achieved by using RASSLs in conjunction with tissue-specific expression systems in vivo. Existing RASSLs have clarified the role of G(i) signaling in cardiac physiology and are currently being used to study cardiomyopathy, muscle remodeling, sensory transduction and complex neurobehavioral responses.

[Indexed for MEDLINE]

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