G protein coupled receptors (GPCRs) represent targets for at least one third of drugs that are cur-rently marketed, and they are of central importance to ongoing drug discovery efforts throughout the pharmaceutical industry. GPCRs contain seven membrane spanning domains and are activated by ligand binding or through other external signaling mechanisms that induce conformational changes in the receptors and lead to activation of associ-ated G proteins and downstream signaling path-ways. The activity of GPCRs is often monitored by quantifying intracellular levels of second messen-gers, such as calcium or cyclic AMP (cAMP).
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