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Article

Structural Insights into β-arrestin/CB1 Receptor Interaction: NMR and CD Studies on Model Peptides

1
Departamento de Química Física Biológica, Instituto de Química Física Rocasolano (IQFR-CSIC), Serrano 119, 28006 Madrid, Spain
2
Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid, Spain
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(21), 8111; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218111
Received: 15 September 2020 / Revised: 21 October 2020 / Accepted: 28 October 2020 / Published: 30 October 2020
Activation of the cannabinoid CB1 receptor induces different cellular signaling cascades through coupling to different effector proteins (G-proteins and β-arrestins), triggering numerous therapeutic effects. Conformational changes and rearrangements at the intracellular domain of this GPCR receptor that accompany ligand binding dictate the signaling pathways. The GPCR-binding interface for G proteins has been extensively studied, whereas β-arrestin/GPCR complexes are still poorly understood. To gain knowledge in this direction, we designed peptides that mimic the motifs involved in the putative interacting region: β-arrestin1 finger loop and the transmembrane helix 7-helix 8 (TMH7-H8) elbow located at the intracellular side of the CB1 receptor. According to circular dichroism and NMR data, these peptides form a native-like, helical conformation and interact with each other in aqueous solution, in the presence of trifluoroethanol, and using zwitterionic detergent micelles as membrane mimics. These results increase our understanding of the binding mode of β-arrestin and CB1 receptor and validate minimalist approaches to structurally comprehend complex protein systems. View Full-Text
Keywords: CB1; β-arrestin1; NMR; Circular dichroism; GPCR CB1; β-arrestin1; NMR; Circular dichroism; GPCR
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MDPI and ACS Style

Morales, P.; Bruix, M.; Jiménez, M.A. Structural Insights into β-arrestin/CB1 Receptor Interaction: NMR and CD Studies on Model Peptides. Int. J. Mol. Sci. 2020, 21, 8111. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218111

AMA Style

Morales P, Bruix M, Jiménez MA. Structural Insights into β-arrestin/CB1 Receptor Interaction: NMR and CD Studies on Model Peptides. International Journal of Molecular Sciences. 2020; 21(21):8111. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218111

Chicago/Turabian Style

Morales, Paula, Marta Bruix, and M. A. Jiménez 2020. "Structural Insights into β-arrestin/CB1 Receptor Interaction: NMR and CD Studies on Model Peptides" International Journal of Molecular Sciences 21, no. 21: 8111. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218111

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