| Evaluation of cAMP Detection Technologies for Screening Gs and Gi Coupled Receptors |
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Presentation: 2B05 Session: Comparing HTS TechnologiesMaite de los Frailes, Francisco Colilla, Emilio Alvarez, Julio Martín, Liz Clark, Rob Slack, Nicola Bevan, Amanda Emmons, Ryan Bingham and James P Villa, GSK Presenting Author: Maite de los Frailes, GSK - Spain Cyclic adenosine monophosphate (cAMP) is an important second messenger that mediates diverse physiological responses of neurotransmitters and hormones. Intracellular cAMP concentration varies upon activation of 7TM Gs and Gi coupled receptors. Many of these receptors are primary targets for a large variety of diseases. The measurement of intracellular cAMP concentration is a commonly used tool for the pharmacological characterization of Gs and Gi coupled receptors, and also a technique for 'screening' them against large libraries of chemical compounds. Low assay sensitivity, high compounds interference or the use of radioactivity, are some of the limitations associated with traditional cAMP methods. In this presentation, we will show data comparing different cAMP detection technologies in terms of sensitivity, robustness, compounds interferences and feasibility to miniaturization and automation. Also, data from real HTS campaigns will be presented. |