All Outputs (7)

Detection and quantification of allosteric modulation of endogenous M4 muscarinic acetylcholine receptor using impedance-based label-free technology in a neuronal cell line (2014)
Journal Article
Chen, A. N., Chen, A., Malone, D. T., Pabreja, K., Sexton, P. M., Christopoulos, A., & Canals, M. (2014). Detection and quantification of allosteric modulation of endogenous M4 muscarinic acetylcholine receptor using impedance-based label-free technology in a neuronal cell line. Journal of Biomolecular Screening, 20(5), 646-654. https://doi.org/10.1177/1087057114563025

© 2014 Society for Laboratory Automation and Screening. Allosteric modulators of G protein-coupled receptors have the potential to achieve greater receptor subtype selectivity compared with ligands targeting the orthosteric site of this receptor fami... Read More about Detection and quantification of allosteric modulation of endogenous M4 muscarinic acetylcholine receptor using impedance-based label-free technology in a neuronal cell line.

Structural basis of receptor sulfotyrosine recognition by a cc chemokine: The n-terminal region of CCR3 bound to CCL11/eotaxin-1 (2014)
Journal Article
Millard, C. J., Ludeman, J. P., Canals, M., Bridgford, J. L., Hinds, M. G., Clayton, D. J., …Stone, M. J. (2014). Structural basis of receptor sulfotyrosine recognition by a cc chemokine: The n-terminal region of CCR3 bound to CCL11/eotaxin-1. Structure, 22(11), 1571-1581. https://doi.org/10.1016/j.str.2014.08.023

© 2014 Elsevier Ltd. Trafficking of leukocytes in immune surveillance and inflammatory responses is activated by chemokines engaging their receptors. Sulfation of tyrosine residues in peptides derived from the eosinophil chemokine receptor CCR3 drama... Read More about Structural basis of receptor sulfotyrosine recognition by a cc chemokine: The n-terminal region of CCR3 bound to CCL11/eotaxin-1.

Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor (2014)
Journal Article
Abdul-Ridha, A., Lane, J. R., Mistry, S. N., Lopez, L., Sexton, P. M., Scammells, P. J., …Canals, M. (2014). Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor. Journal of Biological Chemistry, 289(48), 33701-33711. https://doi.org/10.1074/jbc.m114.604967

Benzylquinolone carboxylic acid (BQCA) is the first highly selective positive allosteric modulator (PAM) for the M1 muscarinic acetylcholine receptor (mAChR), but it possesses low affinity for the allosteric site on the receptor. More recent drug dis... Read More about Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor.

Endothelin-converting enzyme 1 and ?-arrestins exert spatiotemporal control of substance P-induced inflammatory signals (2014)
Journal Article
Jensen, D. D., Halls, M. L., Murphy, J. E., Canals, M., Cattaruzza, F., Poole, D. P., …Bunnett, N. W. (2014). Endothelin-converting enzyme 1 and β-arrestins exert spatiotemporal control of substance P-induced inflammatory signals. Journal of Biological Chemistry, 289(29), 20283-20294. https://doi.org/10.1074/jbc.M114.578179

Although the intracellular trafficking of G protein-coupled receptors controls specific signaling events, it is unclear how the spatiotemporal control of signaling contributes to complex pathophysiological processes such as inflammation. By using bio... Read More about Endothelin-converting enzyme 1 and ?-arrestins exert spatiotemporal control of substance P-induced inflammatory signals.

Novel GPCR paradigms at the ?-opioid receptor (2014)
Journal Article
Thompson, G. L., Kelly, E., Christopoulos, A., & Canals, M. (2015). Novel GPCR paradigms at the ?-opioid receptor. British Journal of Pharmacology, 172(2), 287-296. https://doi.org/10.1111/bph.12600

© 2014 The British Pharmacological Society. Opioids, such as morphine, are the most clinically useful class of analgesic drugs for the treatment of acute and chronic pain. However, the use of opioids is greatly limited by the development of severe ad... Read More about Novel GPCR paradigms at the ?-opioid receptor.

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking (2014)
Journal Article
Yeatman, H. R., Lane, J. R., Choy, K. H. C., Lambert, N. A., Sexton, P. M., Christopoulos, A., & Canals, M. (2014). Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. Journal of Biological Chemistry, 289(22), 15856-15866. https://doi.org/10.1074/jbc.M113.536672

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... Read More about Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking.

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor (2014)
Journal Article
Abdul-Ridha, A., López, L., Keov, P., Thal, D. M., Mistry, S. N., Sexton, P. M., …Christopoulos, A. (2014). Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry, 289(9), 6067-6079. https://doi.org/10.1074/jbc.M113.539080

Benzylquinolone carboxylic acid (BQCA) is an unprecedented example of a selective positive allosteric modulator of acetylcholine at the M1 muscarinic acetylcholine receptor (mAChR). To probe the structural basis underlying its selectivity, we utilize... Read More about Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.