G Protein-Coupled Receptors in Drug Discovery

Volume 552 of the series Methods in Molecular Biology pp 39-50


GPCR Signaling: Understanding the Pathway to Successful Drug Discovery

  • Christine WilliamsAffiliated withDirector HTS CoE, Pfizer Global Research and Development
  • , Stephen J. HillAffiliated withInstitute of Cell Signalling, Queen’s Medical Centre

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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.

Key words

Signaling G protein G protein-coupled receptor Screen Drug discovery