Profiling of G protein-coupled receptor (GPCR) stimulation by small compounds in live cells

Application Note #170

Stimulation of β2-adrenoceptor with epinephrine results in the activation of Gs pathways, while bradykinin B2 receptor activates Gq pathways.

G protein-coupled receptors (GPCRs) are a large family of transmembrane  proteins which are involved in many physiological and pathological processes. Extracellular stimuli result in cellular responses, which lead to ordered and dynamic redistribution of intracellular contents. Cellular responses are receptor-type specific. Accordingly, GPCRs are divided into four subclasses, Gi/o, Gq/11, Gs, and G12/13.

Real-time label-free cell assays provide subtype-specific profiles without the requirement of labeling. However, available assays are based on a multiple-step analysis with additional antagonists or other response-modifying agents, which is especially problematic in cases where the antagonist for a specific pathway is yet to be discovered.

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