Modeling of G-protein-coupled Receptor Signaling Pathways*

G-protein-coupled receptors (GPCRs)2 are the largest family of cell membrane receptors. An estimated 50% of current pharmaceuticals target GPCRs (1), suggesting that further increases in our understanding ofGPCRs and the signaling pathways they initiate will lead to new drug targets. Mathematical and computationalmodeling (here, simply “modeling”) has a substantial history in modern biology and pharmacology (2, 3) and offers a powerful tool for examining GPCR pathways. Such models can be used to better understand hypothesized mechanisms, run virtual (in silico) experiments, interpret data, suggest new drug targets, motivate experiments, and offer new explanations for observed phenomena.

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