All Outputs (6)

Distribution and trafficking of the μ-opioid receptor in enteric neurons of the guinea pig (2016)
Journal Article
Lay, J., Carbone, S. E., DiCello, J. J., Bunnett, N. W., Canals, M., & Poole, D. P. (2016). Distribution and trafficking of the μ-opioid receptor in enteric neurons of the guinea pig. AJP - Gastrointestinal and Liver Physiology, 311(2), G252-G266. https://doi.org/10.1152/ajpgi.00184.2016

© 2016 the American Physiological Society. The μ-opioid receptor (MOR) is a major regulator of gastrointestinal motility and secretion and mediates opiate-induced bowel dysfunction. Although MOR is of physiological and therapeutic importance to gut f... Read More about Distribution and trafficking of the μ-opioid receptor in enteric neurons of the guinea pig.

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor (2016)
Journal Article
Thompson, G., Lane, J., Coudrat, T., Sexton, P., Christopoulos, A., & Canals, M. (2016). Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor. Biochemical Pharmacology, 113, 70-87. https://doi.org/10.1016/j.bcp.2016.05.014

Biased agonism describes the ability of distinct G protein-coupled receptor (GPCR) ligands to stabilise distinct receptor conformations leading to the activation of different cell signalling pathways that can deliver different physiologic outcomes. T... Read More about Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor.

Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the golgi apparatus to the plasma membrane (2016)
Journal Article
Jensen, D. D., Zhao, P., Jimenez-Vargas, N. N., Lieu, T. M., Gerges, M., Yeatman, H. R., Canals, M., Vanner, S. J., Poole, D. P., & Bunnett, N. W. (2016). Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the golgi apparatus to the plasma membrane. Journal of Biological Chemistry, 291(21), 11285-11299. https://doi.org/10.1074/jbc.M115.710681

Agonist-evoked endocytosis of G protein-coupled receptors has been extensively studied. The mechanisms by which agonists stimulate mobilization and plasma membrane translocation of G protein-coupled receptors from intracellular stores are unexplored.... Read More about Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the golgi apparatus to the plasma membrane.

The role of kinetic context in apparent biased agonism at GPCRs (2016)
Journal Article
Javitch, J. A., Klein Herenbrink, C., Sykes, D. A., Donthamsetti, P., Canals, M., Coudrat, T., Shonberg, J., Scammells, P. J., Capuano, B., Sexton, P. M., Charlton, S. J., Javitch, J., Christopoulos, A., & Lane, J. R. (2016). The role of kinetic context in apparent biased agonism at GPCRs. Nature Communications, 7, Article 10842. https://doi.org/10.1038/ncomms10842

Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific drugs that avoid on-target side effects. This mechanism is usu... Read More about The role of kinetic context in apparent biased agonism at GPCRs.

Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors (2016)
Journal Article
Shang, Y., Yeatman, H., Provasi, D., Alt, A., Christopoulos, A., Canals, M., & Filizola, M. (2016). Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors. ACS Chemical Biology, 11(5), 1220-1229. https://doi.org/10.1021/acschembio.5b00712

Available crystal structures of opioid receptors provide a high-resolution picture of ligand binding at the primary ("orthosteric") site, that is, the site targeted by endogenous ligands. Recently, positive allosteric modulators of opioid receptors h... Read More about Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors.

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling (2016)
Journal Article
Halls, M., Yeatman, H., Nowell, C., Thompson, G., Gondin, A., Civciristov, S., Bunnett, N., Lambert, N., Poole, D., & Canals, M. (2016). Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling. Science Signaling, 9(414), ra16-ra16. https://doi.org/10.1126/scisignal.aac9177

Differential regulation of the μ-opioid receptor (MOR), a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor, contributes to the clinically limiting effects of opioid analgesics, such as morphine. We used biophysical appro... Read More about Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling.