Insights into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; advantages and pitfalls of differing methodologies

Stephen J. Hill, Christine Williams, Lauren T. May

Research output: Contribution to journalReview ArticleResearchpeer-review

41 Citations (Scopus)

Abstract

It is clear that the G protein-coupled receptor family play a key role in the pharmaceutical industry, with a significant proportion of approved drugs targeting this protein class. While our growing understanding of the complexity of G protein-coupled receptor pharmacology is playing a key role in the future success of these endeavours, with allosteric mechanisms now well integrated into the industrial community and G protein-independent signalling mechanisms establishing themselves as novel phenomenon to be exploited, it is still possible to underestimate the complexity of G protein signal transduction mechanisms and the impact that inappropriate study of these mechanisms can have on data interpretation. In this manuscript we review different approaches to measuring the cAMP signal transduction pathway, with particular emphasis on key parameters influencing the data quality and biological relevance.

Original languageEnglish
Pages (from-to)1266-1275
Number of pages10
JournalBritish Journal of Pharmacology
Volume161
Issue number6
DOIs
Publication statusPublished - Nov 2010
Externally publishedYes

Keywords

  • CAMP
  • Drug discovery
  • G protein-coupled receptor
  • Screen
  • Signalling

Cite this