Structural studies of opioid receptor activation - GFPP
illicit opioid drugs (opium, heroin) as well as approved therapeutics (morphine and codeine) are mediated by the activation of the mu-opioid receptor (µOR).
19ème Congrès du Groupe Français des Peptides et des Protéines 17-22 mai 2015 Portbail, Normandie, France
Structural studies of opioid receptor activation Sébastien Granier Institut de Génomique Fonctionnelle, Inserm U1191, CNRS UMR 5203, Université de Montpellier, 141 rue de la cardonille, 34094 Montpellier, France.
Opioid receptors (OR), members of the G protein-coupled receptor (GPCR) superfamily, constitute the major and the most effective target for the treatment of pain. Both beneficial and adverse effects of illicit opioid drugs (opium, heroin) as well as approved therapeutics (morphine and codeine) are mediated by the activation of the mu-opioid receptor (µOR). We recently described the structure of an inactive conformation of the µOR. It provided important information regarding the binding site of small morphinan antagonists, revealed a largely exposed binding pocket, and demonstrated key molecular determinants for antagonist binding preferences for OR. However, much remains to be learned about the mechanisms by which different agonists can induce distinct levels of Gi protein activation and/or arrestin recruitment upon activation of µOR. In this study, we propose to analyse the activation mechanism of the µOR using liquid-state NMR spectroscopy and X-ray crystallography. Our goal is to provide insights into opioid receptor activation upon binding of ligands presenting distinct efficacy and/or biased signaling properties. A better knowledge of the structural basis for opioid drug efficacy may lead to new therapeutic approaches with limited side effects.
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