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Journal of Biomolecular Screening
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Article

Duplexed Label-Free G Protein–Coupled Receptor Assays for High-Throughput Screening

Elizabeth Tran and Ye Fang*

* To whom correspondence should be addressed. E-mail: fangy2{at}corning.com.


  Abstract
This article describes duplexed label-free optical biosensor cellular assays for simultaneously assaying 2 endogenous receptors, the Gq-coupled histamine receptor (H1) and the Gs-coupled {beta}2-adrenergic receptor ({beta}2AR), in A431 cells. The biosensor cellular assays consist of 2 sequential steps—an initial agonist screening using Sigma LOPAC (Library of Pharmaceutically Active Compounds) and a subsequent antagonist screening using a solution mixture containing the H1 agonist histamine and the {beta}2AR agonist epinephrine. Results showed that costimulating A431 cells with histamine and epinephrine led to an optical response additive to individual responses. The agonist screening not only identified all full agonists for both the H1 and {beta}2 receptors, but also detected pathway-biased ligands for the {beta}2AR. Furthermore, the succeeding antagonist screening documented all known antagonists in the library for either the H1 or {beta}2 receptors. This is the 1st demonstration of a single cellular assay that is capable of screening ligands against 2 GPCRs coupled to distinct G proteins, and highlights the power of pathway-unbiased and label-free biosensor cellular assays for GPCR screens. (Journal of Biomolecular Screening XXXX:xx-xx)

First published on November 21, 2008, doi:10.1177/1087057108326141

Journal of Biomolecular Screening 2008;13:975.

A more recent version of this article appeared on December 1, 2008

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