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G Protein Signaling: Methods and Protocols (Methods in Molecular Biology, 237),Used
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Since the initial discovery of the G proteincoupled receptor system that regulates cyclicAMP production, the G protein field has rapidly expanded. Cell surface receptors that couple to heterotrimeric G proteins, the G prote coupled receptors (GPCRs), number in the hundreds and bind to a wide div sity of ligands including, biogenic amines (e. g., adrenaline), lipid derivatives (e. g., lysophosphatidic acid), peptides (e. g., opioid peptides), proteins (e. g., thyroidstimulating hormone), and odorants to name a few. The GPCR system is found throughout biology in such simple organisms as yeast and in such more complex organisms as Dictyostelium discoideum (slime mold), Caen habditis elegans (nematode worm), and of course in humans. GPCRs and their associated G protein systems are the subject of intense academic research and because of their involvement in a human biology and disease, the pharmac tical industry has large research initiatives dedicated to the study of GPCRs. By some estimates, more than 50% of the pharmaceuticals on the market are targeted at GPCRs. The G protein/G proteincoupled receptor system consists of a receptor (GPCR), a heterotrimeric G protein consisting of ?, ?, and ? subunits, and an effector. G protein effector molecules, such as enzymes or ion channels, respond to acti tion by the G protein to generate second messengers or changes in membrane potential that lead to alterations in cell physiology.
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