title: Label-Free Cell Phenotypic Assays for Assessing Drug Polypharmacology.
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.
authors.forename: Jixia
authors.initials: J
authors.lastname: Wang
authors.forename: Xiuli
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Incorporated, Corning, New York 14831, USA. fangy2@corning.com.
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
authors.affiliation: Key Laboratory of Separation Science for Analytical Chemistry, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, Liaoning, China. liangxm@dicp.ac.cn.
authors.forename: Xinmiao
authors.initials: X
authors.lastname: Liang
mesh_terms: D000818:Animals; D015374:Biosensing Techniques; D006801:Humans; D004364:Pharmaceutical Preparations; D010641:Phenotype; D064798:Polypharmacology
chemical_list: D004364:Pharmaceutical Preparations