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New Insights into GPCR Function: Implications for HTS

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G Protein-Coupled Receptors in Drug Discovery

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

Summary

G protein-coupled receptors (GPCRs) are a large family of proteins that represent targets for approximately 40% of all approved drugs. They possess unique structural motifs that allow them to interact with a diverse series of extracellular ligands, as well as intracellular signaling proteins, such as G proteins, RAMPs, arrestins, and indeed other receptors. Extensive efforts are under way to discover new generations of drugs against GPCRs with unique targeted therapeutic uses, including “designer” drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.

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Author information

Authors and Affiliations

  1. Bio-discovery, PerkinElmer Life and Analytical Sciences, Waltham, MA, USA

    Richard M. Eglen

  2. Independent consultant, Los Angeles, CA, USA

    Terry Reisine

Authors
  1. Richard M. Eglen
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  2. Terry Reisine
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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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Eglen, R.M., Reisine, T. (2009). New Insights into GPCR Function: Implications for HTS. 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_1

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  • DOI: https://doi.org/10.1007/978-1-60327-317-6_1

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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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