%0 Journal Article
%T Label-free drug discovery
%A Ye Fang
%J Frontiers in Pharmacology
%D 2014
%I Frontiers Media
%R 10.3389/fphar.2014.00052
%X Current drug discovery is dominated by label-dependent molecular approaches, which screen drugs in the context of a predefined and target-based hypothesis in vitro. Given that target-based discovery has not transformed the industry, phenotypic screen that identifies drugs based on a specific phenotype of cells, tissues, or animals has gained renewed interest. However, owing to the intrinsic complexity in drug¨Ctarget interactions, there is often a significant gap between the phenotype screened and the ultimate molecular mechanism of action sought. This paper presents a label-free strategy for early drug discovery. This strategy combines label-free cell phenotypic profiling with computational approaches, and holds promise to bridge the gap by offering a kinetic and holistic representation of the functional consequences of drugs in disease relevant cells that is amenable to mechanistic deconvolution.
%K cell phenotypic screen
%K drug safety/toxicity
%K label-free drug discovery
%K lead selection
%K molecular mechanism of action
%K phenotypic screen
%K polypharmacology
%K target identification
%U http://www.frontiersin.org/Journal/10.3389/fphar.2014.00052/abstract