Label-Free Cell Phenotypic Assays for Assessing Drug Polypharmacology

Current Pharmaceutical Design
Jixia WangXinmiao Liang

Abstract

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. 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. 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. Label-free cell phenotypic assays hold great potential in assessing drug polypharmacology.

Citations

May 23, 2018·Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences·W GamalP O Bagnaninchi
Nov 30, 2019·Naunyn-Schmiedeberg's Archives of Pharmacology·Lala QuXinmiao Liang

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