Receptor Panning

A unique application enabled by the ability of the CellKey™ System is to reliably quantify activation of endogenous receptors. This application allows investigators to easily screen disease-relevant cell types for functionally active target receptors by treating cells with a panel of generic and receptor-specific ligands, compounds, and peptides that are known to activate different types of receptors.

Changes in impedance related to extracellular current (Ziec) are measured following exposure to these compounds and responses that are outside the threshold of three standard deviations above or below the buffer mean are considered statistically significant and indicative of a functional endogenous receptor.  Three examples of receptor panning are shown in the figure below.

Receptor Panning - CDS responses identify functional endogenous receptors in cells commonly used in drug discovery, HEK293, CHO_m1, and U-2 OS. The change in impedance (Ziec) is plotted in each graph, with a hit set at three standard deviations above and below the buffer mean, as represented by the dotted orange line.

Receptor panning of multiple cell types has resulted in the identification of many functionally active, differently coupled endogenous receptors, some of which have not been previously documented in the literature.  This ability to functionally measure activity of endogenous receptors in a wide variety of cell types enables more physiologically relevant selectivity and specificity screens with the goal of providing more successful drug discovery campaigns.  Furthermore, the receptor panning application can be used to screen and optimize compound libraries.

For More Information

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Application Bulletin

Application Bulletin 1: Receptor Panning *

Brochure

CellKey System Brochure *

Poster

A Label-free Cell-based Assay Technology for Functional Evaluation of Endogenous Receptors *

Identification of the G-protein Coupling Mechanism of GPCRs Using a Label-free Live-Cell Assay *

Cataloging Endogenous Cell Surface Receptors and Analyzing Their Functional Activity using Label-Free Cellular Dielectric Spectroscopy

Investigating the FcERI Receptor Signaling Pathway and Mast Cell Degranulation Using a Novel Label-Free Cell-Based Assay Technology *

Other Applications

Hit Identification and Pharmalogical Profiling

Signal Pathway Identification and Deconvolution