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All Outputs (7)

GRKs as Key Modulators of Opioid Receptor Function (2020)
Journal Article
Lemel, L., Lane, J. R., & Canals, M. (2020). GRKs as Key Modulators of Opioid Receptor Function. Cells, 9(11), Article 2400. https://doi.org/10.3390/cells9112400

Understanding the link between agonist-induced phosphorylation of the mu-opioid receptor (MOR) and the associated physiological effects is critical for the development of novel analgesic drugs and is particularly important for understanding the mecha... Read More about GRKs as Key Modulators of Opioid Receptor Function.

The life cycle of the Mu-Opioid Receptor (2020)
Journal Article
Cuitavi, J., Hipólito, L., & Canals, M. (2021). The life cycle of the Mu-Opioid Receptor. Trends in Biochemical Sciences, 46(4), 315-328. https://doi.org/10.1016/j.tibs.2020.10.002

Opioid receptors are undisputed targets for the treatment of pain. Unfortunately, targeting these receptors therapeutically poses significant challenges including addiction, dependence, tolerance and the appearance of side-effects such as respiratory... Read More about The life cycle of the Mu-Opioid Receptor.

Critical assessment of G protein-biased agonism at the µ opioid receptor (2020)
Journal Article
Gillis, A., Kliewer, A., Kelly, E., Henderson, G., Christie, M. J., Schulz, S., & Canals, M. (2020). Critical assessment of G protein-biased agonism at the µ opioid receptor. Trends in Pharmacological Sciences, 41(12), 947-959. https://doi.org/10.1016/j.tips.2020.09.009

G protein-biased agonists of the µ-opioid receptor have been proposed to be an improved class of opioid analgesics. Recent studies have been unable to reproduce the original experiments in the β-arrestin2 knockout mouse that led to this proposal, and... Read More about Critical assessment of G protein-biased agonism at the µ opioid receptor.

Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2 (2020)
Journal Article
Huang, C., Foster, S. R., Shah, A. D., Kleifeld, O., Canals, M., Schittenhelm, R. B., & Stone, M. J. (2020). Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2. Journal of Biological Chemistry, 295, 6518-6531. https://doi.org/10.1074/jbc.ra119.012026

Leukocyte recruitment is a universal feature of tissue inflammation and regulated by the interactions of chemokines with their G protein-coupled receptors (GPCRs). Activation of CC chemokine receptor 2 (CCR2) by its cognate chemokine ligands, includi... Read More about Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2.

Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists (2020)
Journal Article
Gillis, A., Gondin, A. B., Kliewer, A., Sanchez, J., Lim, H. D., Alamein, C., …Canals, M. (2020). Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists. Science Signaling, 13(625), Article eaaz3140. https://doi.org/10.1126/scisignal.aaz3140

Biased agonism at G protein–coupled receptors describes the phenomenon whereby some drugs can activate some downstream signaling activities to the relative exclusion of others. Descriptions of biased agonism focusing on the differential engagement of... Read More about Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists.