Label-Free Cell Phenotypic Assays for Assessing Drug Polypharmacology

Author(s): Jixia Wang, Xiuli Zhang, Ye Fang, Xinmiao Liang

Journal Name: Current Pharmaceutical Design

Volume 22 , Issue 21 , 2016

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Background: Most drugs exert their biological and physiological effects via binding to protein targets. Although drugs are traditionally optimized against a single protein, most marketed drugs exhibit clinically relevant polypharmacology – the activity of drugs at multiple targets. The wide-spread presence of polypharmacology makes it challenging to assess the mechanisms of action of multi-target drugs. Methods: This paper first reviews approaches for discovering multi-targets of drug molecules, then discusses key characteristics of label-free cell phenotypic assays, and finally focuses on how to use these assays to assess drug polypharmacology. Results: labelfree cell phenotypic assays have ability to provide a holistic view of drug action in living cells with wide phenotype/ target/pathway coverage, and permit effective deconvolution of the action of multi-target drugs at the whole cell level. Conclusion: Label-free cell phenotypic assays hold great potential in assessing drug polypharmacology.

Keywords: label-free cell phenotypic assay, mechanism of action, multi-target screen, polypharmacology, resonant waveguide grating biosensor, electric biosensor.

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Article Details

Year: 2016
Published on: 24 February, 2016
Page: [3190 - 3200]
Pages: 11
DOI: 10.2174/1381612822666160224142048
Price: $65

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