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High-Throughput Lead Finding and Optimisation for GPCR Targets

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GPCRs: From Deorphanization to Lead Structure Identification

Part of the book series: Ernst Schering Foundation Symposium Proceedings ((SCHERING FOUND,volume 2006/2))

Abstract

Driven by past successes and the detailed knowledge of signalling cascades and physiological processes, G-protein-coupled receptors are taking a prominent place in the portfolios of many pharmaceutical companies. To successfully address this target class, scientists need not only a good understanding of the specific receptor under investigation, but also the right tools from assay technology, reagent production to a hit-to-lead process that acknowledges the importance of parameters beyond potency and embraces the gain in knowledge of the last decade. This manuscripts attempts to summarise some of the changes and progress made across the pharmaceutical industry to design an efficient and effective strategy for finding and optimising small molecules modulating the activity of GPCRs.

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Authors and Affiliations

  1. Primary Pharmacology Group, Pfizer PDGRD, IPC 580, Ramsgate Road, CT13 9NJ, Sandwich, UK

    A. Sewing & D. Cawkill

Authors
  1. A. Sewing
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  2. D. Cawkill
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Corresponding author

Correspondence to A. Sewing .

Editor information

H. Bourne R. Horuk J. Kuhnke H. Michel

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© 2007 Springer-Verlag

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Sewing, A., Cawkill, D. (2007). High-Throughput Lead Finding and Optimisation for GPCR Targets. In: Bourne, H., Horuk, R., Kuhnke, J., Michel, H. (eds) GPCRs: From Deorphanization to Lead Structure Identification. Ernst Schering Foundation Symposium Proceedings, vol 2006/2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/2789_2006_012

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