All Outputs (8)

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1 (2018)
Journal Article
Sanchez, J., e Huma, Z., Lane, J., Liu, X., Bridgford, J. L., Payne, R. J., …Stone, M. J. (2018). Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1. Journal of Biological Chemistry, 294(10), 3464-3475. https://doi.org/10.1074/jbc.ra118.006535

© 2019 Sanchez et al. Published under exclusive license by The American Society for Biochemistry and Molecular Biology, Inc. Interactions between secreted immune proteins called chemokines and their cognate G protein– coupled receptors regulate the t... Read More about Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1.

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations (2018)
Journal Article
Civciristov, S., Ellisdon, A. M., Suderman, R., Pon, C. K., Evans, B. A., Kleifeld, O., …Halls, M. L. (2018). Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations. Science Signaling, 11(551), Article eaan1188. https://doi.org/10.1126/scisignal.aan1188

G protein–coupled receptors (GPCRs) are the largest class of cell surface signaling proteins, participate in nearly all physiological processes, and are the targets of 30% of marketed drugs. Typically, nanomolar to micromolar concentrations of ligand... Read More about Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations.

Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon (2018)
Journal Article
Dicello, J., Saito, A., Rajasekhar, P., Eriksson, E., McQuade, R., Nowell, C., …Poole, D. (2018). Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon. American Journal of Physiology, 315(4), G544-G559. https://doi.org/10.1152/ajpgi.00025.2018

Endoge-nous opioids activate opioid receptors (ORs) in the enteric nervous system to control intestinal motility and secretion. The μ-OR mediates the deleterious side effects of opioid analgesics, including constipation, respiratory depression, and a... Read More about Hormones, neurotransmitters, growth factors, receptors, and signaling: Inflammation-associated changes in DOR expression and function in the mouse colon.

Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid -opioid receptor desensitization (2018)
Journal Article
Miess, E., Gondin, A. B., Yousuf, A., Steinborn, R., Mösslein, N., Yang, Y., …Canals, M. (2018). Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid -opioid receptor desensitization. Science Signaling, 11(539), Article eaas9609. https://doi.org/10.1126/scisignal.aas9609

Copyright © 2018 The Authors. G protein receptor kinases (GRKs) and -arrestins are key regulators of -opioid receptor (MOR) signaling and trafficking. We have previously shown that high-efficacy opioids such as DAMGO stimulate a GRK2/3-mediated multi... Read More about Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid -opioid receptor desensitization.

Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome (2018)
Journal Article
Jimenez-Vargas, N. N., Pattison, L. A., Zhao, P., Lieu, T. M., Latorre, R., Jensen, D. D., …Bunnett, N. W. (2018). Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome. Proceedings of the National Academy of Sciences, 115(31), E7438-E7447. https://doi.org/10.1073/pnas.1721891115

© 2018 National Academy of Sciences. All rights reserved. Once activated at the surface of cells, G protein-coupled receptors (GPCRs) redistribute to endosomes, where they can continue to signal. Whether GPCRs in endosomes generate signals that contr... Read More about Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome.

Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization (2018)
Journal Article
Huang, C., Lewis, C., Borg, N. A., Canals, M., Diep, H., Drummond, G. R., …Stone, M. J. (2018). Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization. Journal of Proteome Research, 17(4), 1485-1499. https://doi.org/10.1021/acs.jproteome.7b00828

Macrophages, which accumulate in tissues during inflammation, may be polarized toward pro-inflammatory (M1) or tissue reparative (M2) phenotypes. The balance between these phenotypes can have a substantial influence on the outcome of inflammatory dis... Read More about Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization.

Pharmacologic evidence for a putative conserved allosteric site on opioid receptors (2018)
Journal Article
Livingston, K., Stanczyk, M., Burford, N., Alt, A., Canals, M., & Traynor, J. (2018). Pharmacologic evidence for a putative conserved allosteric site on opioid receptors. Molecular Pharmacology, 93(2), 157-167. https://doi.org/10.1124/mol.117.109561

Allosteric modulators of G protein-coupled receptors, including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the μ-opioid receptor (μ-OR). BMS-98... Read More about Pharmacologic evidence for a putative conserved allosteric site on opioid receptors.

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies (2018)
Journal Article
Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B., & Scammells, P. J. (2018). Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. Journal of Medicinal Chemistry, 61(3), 1316-1329. https://doi.org/10.1021/acs.jmedchem.7b01811

Opioids, like morphine, are the mainstay analgesics for the treatment and control of pain. Despite this, they often exhibit severe side effects that limit dose; patients often become tolerant and dependent on these drugs, which remains a major health... Read More about Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.