Identification of therapeutic small-molecule leads in cultured cells using multiplexed pathway reporter readouts

Ozlem Kulak, Kiyoshi Yamaguchi, Lawrence Lum

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

The rapid expansion of molecular screening libraries in size and complexity in the last decade has outpaced the discovery rate of cost-effective strategies to single out reagents with sought-after cellular activities. In addition to representing high-priority therapeutic targets, intensely studied cell signaling systems encapsulate robust reference points for mapping novel chemical activities given our deep understanding of the molecular mechanisms that support their activity. In this chapter, we describe strategies for using transcriptional reporters of several well-interrogated signal transduction pathways coupled with high-throughput biochemical assays to fingerprint novel compounds for drug target identification agendas.

Original languageEnglish (US)
Pages (from-to)3-16
Number of pages14
JournalMethods in Molecular Biology
Volume1263
DOIs
StatePublished - 2015

Keywords

  • Dot blotting
  • Kras
  • Luciferase assay
  • RNAi
  • Small-molecule screening
  • TP53
  • Wnt

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics

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