Article
Distinct CCK-2 receptor conformations associated with β-arrestin-2 recruitment or phospholipase-C activation revealed by a biased antagonist.
Journal of the American Chemical Society - 20 Feb 2013
Magnan Rémi, Escrieut Chantal, Gigoux Véronique, De Kavita, Clerc Pascal, Niu Fan, Azema Joelle, Masri Bernard, Cordomi Arnau, Baltas Michel, Tikhonova Irina G, Fourmy Daniel
Abstract excerpt
Seven-transmembrane receptors (7TMRs), also termed G protein-coupled receptors (GPCRs), form the largest class of cell surface membrane receptors, involving several hundred members in the human genome. Nearly 30% of marketed pharmacological agents target 7TMRs. 7TMRs adopt multiple conformations upon agonist binding. Biased agonists, in contrast to non-biased agonists, are believed to stabilize conformations...
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