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Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development

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Part of the book series: Methods in Molecular Biology ((MIMB,volume 986))

Abstract

Cellular models for siRNA and small molecule high throughput screening have been widely used in the last decade to identify targets for drug discovery. As an example, we present a two-fold readout approach based on cell viability and multipolar phenotype. To maximize the discovery of potential targets and at the same time reduce the number of false positives in our dataset, we have combined focused and rationally designed custom siRNA libraries with small molecule inhibitor libraries. Here we describe a cellular model for centrosome amplification as an example of how to design and perform a multiple readout/multiple screening strategy.

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References

  1. Westwick JK, Lamerdin JE (2011) Improving drug discovery with contextual assays and cellular systems analysis. Methods Mol Biol 756:61–73

    Article  PubMed  CAS  Google Scholar 

  2. Dezso Z, Nikolsky Y, Nikolskaya T et al (2009) Identifying disease-specific genes based on their topological significance in protein networks. BMC Syst Biol 23:3–36

    Google Scholar 

  3. Ashworth A, Bernards R (2010) Using functional genetics to understand breast cancer biology. Cold Spring Harb Perspect Biol 2:a003327

    Article  PubMed  Google Scholar 

  4. Nigg EA, Stearns T (2011) The centrosome cycle: centriole biogenesis, duplication and inherent asymmetries. Nat Cell Biol 13:1154–1160

    Article  PubMed  CAS  Google Scholar 

  5. Kwon M, Godinho SA, Chandhok NS et al (2008) Mechanisms to suppress multipolar divisions in cancer cells with extra centrosomes. Genes Dev 22:2189–2203

    Article  PubMed  CAS  Google Scholar 

  6. Zhang XD, Yang XC, Chung N et al (2006) Robust statistical methods for hit selection in RNA interference high-throughput screening experiments. Pharmacogenomics 7:299–309

    Article  PubMed  CAS  Google Scholar 

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Drosopoulos, K., Linardopoulos, S. (2013). Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development. In: Moll, J., Colombo, R. (eds) Target Identification and Validation in Drug Discovery. Methods in Molecular Biology, vol 986. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-311-4_7

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  • DOI: https://doi.org/10.1007/978-1-62703-311-4_7

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  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-62703-310-7

  • Online ISBN: 978-1-62703-311-4

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