All Outputs (6)

A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor (2019)
Journal Article
Dekan, Z., Sianati, S., Yousuf, A., Sutcliffe, K. J., Gillis, A., Mallet, C., …Christie, M. J. (2019). A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor. Proceedings of the National Academy of Sciences, 116(44), 22353-22358. https://doi.org/10.1073/pnas.1908662116

An Australian estuarine isolate ofPenicilliumsp. MST-MF667 yielded3 tetrapeptides named the bilaids with an unusual alternating LDLDchirality. Given their resemblance to known short peptide opioidagonists, we elucidated that they were weak (Kilow mic... Read More about A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor.

Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks (2019)
Journal Article
Civciristov, S., Huang, C., Liu, B., Marquez, E. A., Gondin, A. B., Schittenhelm, R. B., …Halls, M. L. (2019). Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks. Journal of Biological Chemistry, 294(44), 16198-16213. https://doi.org/10.1074/jbc.ra119.008685

Ligand-dependent differences in the regulation and internalization of the mu-opioid receptor (MOR) have been linked to the severity of adverse effects that limit opiate use in pain management. MOR activation by morphine or [D-Ala2,N-MePhe4,Gly-ol]-en... Read More about Ligand-dependent spatiotemporal signaling profiles of the mu-opioid receptor are controlled by distinct protein-interaction networks.

Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1 (2019)
Journal Article
Sanchez, J., Lane, R., Canals, M., & Stone, M. J. (2019). Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1. International Journal of Molecular Sciences, 20(10), 1-15. https://doi.org/10.3390/ijms20102417

Leukocyte migration, a hallmark of the inflammatory response, is stimulated by the interactions between chemokines, which are expressed in injured or infected tissues, and chemokine receptors, which are G protein-coupled receptors (GPCRs) expressed i... Read More about Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1.

GRK mediates ?-opioid receptor plasma membrane reorganization (2019)
Journal Article
Gondin, A. B., Halls, M. L., Canals, M., & Briddon, S. J. (2019). GRK mediates ?-opioid receptor plasma membrane reorganization. Frontiers in Molecular Neuroscience, 12, https://doi.org/10.3389/fnmol.2019.00104

Differential regulation of the ?-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylati... Read More about GRK mediates ?-opioid receptor plasma membrane reorganization.

G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases (2019)
Journal Article
Canals, M., Poole, D. P., Veldhuis, N. A., Schmidt, B. L., & Bunnett, N. W. (2019). G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases. Gastroenterology, 156(6), 1600-1616. https://doi.org/10.1053/j.gastro.2019.01.266

G protein-coupled receptors (GPCRs) are the largest family of transmembrane signaling proteins. Within the gastrointestinal tract, GPCRs expressed by epithelial cells sense contents of the lumen, and GPCRs expressed by epithelial cells, myocytes, neu... Read More about G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases.

Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer (2019)
Journal Article
Blasco-Benito, S., Moreno, E., Seijo-Vila, M., Tundidor, I., Andradas, C., Caffarel, M. M., …Sánchez, C. (2019). Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer. Proceedings of the National Academy of Sciences, 116(9), 3863-3872. https://doi.org/10.1073/pnas.1815034116

Although human epidermal growth factor receptor 2 (HER2)-targeted therapies have dramatically improved the clinical outcome of HER2-positive breast cancer patients, innate and acquired resistance remains an important clinical challenge. New therapeut... Read More about Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer.