Article
Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.
Scientific reports - 20 Oct 2015
Stornaiuolo Mariano, Bruno Agostino, Botta Lorenzo, La Regina Giuseppe, Cosconati Sandro, Silvestri Romano, Marinelli Luciana, Novellino Ettore
Abstract excerpt
A Cannabinoid Receptor 1 (CB1) binding site for the selective allosteric modulator ORG27569 is here identified through an integrate approach of consensus pocket prediction, mutagenesis studies and Mass Spectrometry. This unprecedented ORG27569 pocket presents the structural features of a Cholesterol Consensus Motif, a cholesterol interacting region already found in other GPCRs. ORG27569 and cholesterol affects...
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