Engineering receptors activated solely by synthetic ligands (RASSLs)

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 sig...

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Bibliographic Details
Published in:Trends in Pharmacological Sciences 2001-08, Vol.22 (8), p.414-420
Main Authors: Scearce-Levie, Kimberly, Coward, Peter, Redfern, Charles H., Conklin, Bruce R.
Format: Article
Language:English
Subjects:
Analgesics - pharmacology
Animals
cardiomyopathy
GPCRs
Heart Rate - drug effects
Humans
Mice
Mice, Transgenic
Pyrrolidines - pharmacology
receptor engineering
Receptors, Cell Surface - drug effects
Receptors, Cell Surface - metabolism
Receptors, Opioid, kappa - agonists
Receptors, Opioid, kappa - metabolism
Receptors, Opioid, kappa - physiology
Recombinant Fusion Proteins
Signal Transduction
Technology, Pharmaceutical
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Summary: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.
ISSN:0165-6147
1873-3735
DOI:10.1016/S0165-6147(00)01743-0