Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
iDDPartners, 3 Edith Court
Princeton Junction
NJ 08550


Label-Free Cell-Based Assays for GPCR Screening

Author(s): Ye Fang, Anthony G. Frutos, Ronald Verklereen.


G protein-coupled receptors (GPCRs) have been proven to be the largest family of druggable targets in the human genome. Given the importance of GPCRs as drug targets and the de-orphanization of novel targets, GPCRs are likely to remain the frequent targets of many drug discovery programs. With recent advances in instrumentation and understanding of cellular mechanisms for the signals measured, biosensor-centered label-free cell assay technologies become a very active area for GPCR screening. This article reviews the principles and potential of current label-free cell assay technologies in GPCR drug discovery.

Keywords: G protein-coupled receptor, optical biosensor, resonant waveguide grating biosensor, electrical biosensor, dynamic mass redistribution, impedance, high throughput screening

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Article Details

Year: 2008
Page: [357 - 369]
Pages: 13
DOI: 10.2174/138620708784534789