Definitions
GPCR – G protein–coupled receptor
Activation – a series of conformational changes in the receptor that leads to activation of intracellular G proteins and other effectors
Agonist – a ligand that, upon binding, stabilizes an active state of the receptor, leading to activation of cytoplasmic effectors and subsequent cellular responses
Inverse agonist – a ligand that, upon binding, stabilizes an inactive state of the receptor, which reduces basal activity
Introduction
G protein–coupled receptors (GPCRs) are seven transmembrane proteins that transmit a wide variety of extracellular signals (photons, odorants, pheromones, biogenic amines, (neuro)peptides, proteases, glycoprotein hormones, and ions) across the plasma membrane. When activated by light or ligands, GPCRs...
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Veprintsev, D., Deupi, X., Standfuss, J., Schertler, G.F.X. (2013). G Protein–Coupled Receptor Activation Based on X-ray Structural Studies. In: Roberts, G.C.K. (eds) Encyclopedia of Biophysics. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-16712-6_785
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DOI: https://doi.org/10.1007/978-3-642-16712-6_785
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