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Dissecting the conserved NPxxY motif of the M3 muscarinic acetylcholine receptor: critical role of Asp-7.49 for receptor signaling and multiprotein complex formation.

Cell Physiol Biochem.. 2011-12;  28(5):1009-12
Dasiel O. Borroto-Escuela, , Wilber Romero-Fernandez, Gloria GarcÍa-Negredo, Patricia A. Correia, Pere Garriga, Kjell Fuxe and Francisco Ciruela. Unitat de Farmacologia, Departament de Patologia i TerapÈutica Experimental, Facultat de Medicina, Universitat de Barcelona, L'Hospitalet de Llobregat
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摘要

Acetylcholine challenge produces M3 muscarinic acetylcholine receptor activation and accessory/scaffold proteins recruitment into a signalsome complex. The dynamics of such a complex is not well understood but a conserved NPxxY motif located within transmembrane 7 and juxtamembrane helix 8 of the receptor was found to modulate G protein activation. Here by means of receptor mutagenesis we unravel the role of the conserved M3 muscarinic acetylcholine receptor NPxxY motif on ligand binding, signaling and multiprotein complex formation. Interestingly, while a N7.49D receptor mutant showed normal ligand binding properties a N7.49A mutant had reduced antagonist binding and increased affinity for carbachol. Also, bes... More

关键词

G protein-coupled receptors; Muscarinic acetylcholine receptors; NPxxY motif; Phospholipase D; Phospholipase C; Monomeric small G proteins; Desensitization.