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GPCR Signaling: Understanding the Pathway to Successful Drug Discovery

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G Protein-Coupled Receptors in Drug Discovery

Part of the book series: Methods in Molecular Biology ((MIMB,volume 552))

Summary

Modulators of G protein-coupled receptors (GPCRs) form a key area for the pharmaceutical industry, representing ˜27% of all Food and Drug Administration (FDA)-approved drugs. Consequently, there are a wide variety of in vitro plate-based screening technologies that enable the measurement of compound affinity, potency, and efficacy for almost every type of GPCR. However, to maximize success it is prudent to ensure that (i) the most suitable assay formats are identified, (ii) they are configured optimally to detect the desired compound activity, and (iii) that they form a basis for predicting clinical effects. To achieve this, an understanding of the pathways and mechanisms of receptor activation relevant to the disease mechanism, as well as the benefits and/or limitations of the specific techniques, is key.

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Author information

Authors and Affiliations

  1. Director HTS CoE, Pfizer Global Research and Development, Sandwich, Kent, UK

    Christine Williams

  2. Institute of Cell Signalling, Queen’s Medical Centre, Nottingham, UK

    Stephen J. Hill

Authors
  1. Christine Williams
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  2. Stephen J. Hill
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Editor information

Editors and Affiliations

  1. CSIRO Human Nutrition, Kintore Ave., Adelaide, 5000, Australia

    Wayne R. Leifert

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© 2009 Humana Press, a part of Springer Science+Business Media, LLC

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Williams, C., Hill, S.J. (2009). GPCR Signaling: Understanding the Pathway to Successful Drug Discovery. In: Leifert, W. (eds) G Protein-Coupled Receptors in Drug Discovery. Methods in Molecular Biology, vol 552. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60327-317-6_3

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  • DOI: https://doi.org/10.1007/978-1-60327-317-6_3

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  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-60327-316-9

  • Online ISBN: 978-1-60327-317-6

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