Ligand-directed signaling, biased agonism, and functional selectivity are terms that describe the propensity of a ligand to drive signaling toward one GPCR pathway over another. Most of the early examples demonstrated to date examine the divergence between GPCR signaling to G protein coupling and βarrestin2 recruitment. As biased agonists begin to become available based on cell-based screening criteria, a need arises to determine if G protein signaling biases will be maintained in the endogenous setting, wherein receptors are functioning to control relevant biological responses. This report presents our method and offers tips for evaluating G protein signaling in endogenous tissues. Predominately, brain tissues are discussed here; optimization points that can be applied to any tissues are highlighted.
CITATION STYLE
Bohn, L. M., Zhou, L., & Ho, J. H. (2015). Approaches to assess functional selectivity in gpcrs: Evaluating g protein signaling in an endogenous environment. Methods in Molecular Biology, 1335, 177–189. https://doi.org/10.1007/978-1-4939-2914-6_12
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