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The application of high-throughput screening to novel lead discovery

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Progress in Drug Research

Part of the book series: Progress in Drug Research ((PDR,volume 51))

Summary

The ability to discover new lead compounds for novel therapeutic targets is a pivotal step in drug discovery programmes. High-throughput screening (HTS) utilises a number of platforms for the rapid screening of novel targets to accelerate this process. Key issues in HTS include assay configuration and the ability of a high-throughput screen to predict drug-target interactions accurately. This review highlights a number of issues in the HTS process and describes three key target areas that are likely to be sources of novel, therapeutically important drugs. Particular emphasis is placed on the mechanistic basis of drug-target interactions that are of prime importance in the design of HTS approaches. Critical aspects of information management related to HTS are summarised.

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Abbreviations

HTS:

high-throughput screening

SPA:

scintillation proximity assay

HTRF:

homogeneous timeresolved fluorescence

ELISA:

enzyme-linked immunoabsorbtion assay

GFP:

green fluorescent protein

RTK:

receptor tyrosine kinases

GPCR:

G-protein-coupled receptor

EGRF:

epidermal growth factor receptor

FRET:

fluorescence resonance energy transfer

CRE:

cyclic-AMP response element

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Author information

Authors and Affiliations

  1. Cambridge Drug Discovery, 3 Brookmount Court Kirkwood Road, Cambridge, CB4 2QH, UK

    Barry A. Kenny, Mark Bushfield, David J. Parry-Smith, Simon Fogarty & J. Mark Treherne

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  1. Barry A. Kenny
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  2. Mark Bushfield
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  3. David J. Parry-Smith
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  4. Simon Fogarty
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  5. J. Mark Treherne
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Editors and Affiliations

  1. Steinweg 28, CH-4107, Ettingen, Switzerland

    Ernst Jucker

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© 1998 Springer Basel AG

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Kenny, B.A., Bushfield, M., Parry-Smith, D.J., Fogarty, S., Treherne, J.M. (1998). The application of high-throughput screening to novel lead discovery. In: Jucker, E. (eds) Progress in Drug Research. Progress in Drug Research, vol 51. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8845-5_7

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  • DOI: https://doi.org/10.1007/978-3-0348-8845-5_7

  • Publisher Name: Birkhäuser, Basel

  • Print ISBN: 978-3-0348-9798-3

  • Online ISBN: 978-3-0348-8845-5

  • eBook Packages: Springer Book Archive

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