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GPCR signalosome: components and actions. GPCRs constitute a large family of transmembrane proteins that transduce extracellular stimuli into intracellular signaling responses. Ligand binding to GPCRs leads to activation of heterotrimeric G alpha (Gα) proteins, which have various downstream effects on intracellular processes. Drug action on GPCRs was reviewed extensively in ref. 35.
