Background: The effects of allosteric modulators on G protein-coupled receptor trafficking are largely unknown. Results: The allosteric ligand BQCA modulates M1 mAChR arrestin recruitment and receptor trafficking. Conclusion: M1 mAChR trafficking is arrestin- and G protein-dependent and modulated by BQCA. Significance: The impact of allosteric modulators on receptor trafficking needs to be assessed when considering this family of ligands as potential chronic therapies. ? 2014 by The American Society for Biochemistry and Molecular Biology, Inc. Published in the U.S.A.
Yeatman, H. R., Lane, J. R. D., Choy, K. H. C., Lambert, N., Sexton, P., Christopoulos, A., & Canals, M. (2014). Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. The Journal of Biological Chemistry, 289(22), 15856 - 15866. https://doi.org/10.1074/jbc.M113.536672