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Nat Methods. 2008 Aug;5(8):673-8. doi: 10.1038/nmeth.1232.

Engineering GPCR signaling pathways with RASSLs.

Author information

  • 1Gladstone Institute of Cardiovascular Disease, 1650 Owens Street, San Francisco, California 94158, USA. bconklin@gladstone.ucsf.edu

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.

PMID:
18668035
[PubMed - indexed for MEDLINE]
PMCID:
PMC2703467
Free PMC Article

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