Engineering GPCR signaling pathways with RASSLs

Academic Article

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Overview

authors

• Conklin, B. R.
• Hsiao, E. C.
• Claeysen, S.
• Dumuis, A.
• Srinivasan, Supriya
• Forsayeth, J. R.
• Guettier, J. M.
• Chang, W. C.
• Pei, Y.
• McCarthy, K. D.
• Nissenson, R. A.
• Wess, J.
• Bockaert, J.
• Roth, B. L.

publication date

• August 2008

journal

• Nature Methods  Journal

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.

subject areas

• Animals
• Evolution, Molecular
• Humans
• Ligands
• Protein Binding
• Protein Engineering
• Receptors, G-Protein-Coupled
• Signal Transduction

Identity

PubMed Central ID

• PMC2703467

International Standard Serial Number (ISSN)

• 1548-7091

Digital Object Identifier (DOI)

• 10.1038/nmeth.1232

PubMed ID

• 18668035

Additional Document Info

start page

• 673

end page

• 678

volume

• 5

issue

• 8