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Editorial

The resurgence of phenotypic screening in drug discovery and development

Pages 121-125 | Received 17 Sep 2015, Accepted 17 Nov 2015, Published online: 10 Dec 2015

References

  • Papers of special note have been highlighted as either of interest (•) or of considerable interest (••) to readers.
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••This important article presents a comprehensive analysis of drug discovery during the 2000s, and makes a case for the importance of phenotype-based discoveries

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•This presentation of a nearly decade-long effort toward antibacterial discovery highlights the limitations of taking a purely target-based approach toward drug discovery

•This work outlines the authors’ recommended criteria in developing an effective phenotypic assay, and emphasizes the importance of using physiologically relevant material and readouts

  • Van Goor F, Hadida S, Grootenhuis PD, et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc Natl Acad Sci USA. 2011;108:18843–18848.
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•This article summarizes the success stories that emerged from the NIH’s MLPCN screening program, and differentiates the characteristics of small-molecule probes and drugs

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•This review provides a good overview of the many techniques necessary to understand small-molecule MoA

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••This article discusses a genomics-based approach toward target validation and drug discovery, arguing that such human “experiments of nature” inspire more confidence in targets for therapeutics development

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