All Outputs (59)

Phosphoproteomic characterization of the signaling network resulting from activation of chemokine receptor CCR2 (2020)
Journal Article

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

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.

Opioid pharmacology under the microscope (2020)
Journal Article

A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor (2019)
Journal Article

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

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

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

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

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

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.

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1 (2018)
Journal Article

© 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

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

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

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

© 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

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

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

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.

Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission (2017)
Journal Article

G protein-coupled receptors (GPCRs) are considered to function primarily at the plasma membrane, where they interact with extracellular ligands and couple to G proteins that transmit intracellular signals. Consequently, therapeutic drugs are designed... Read More about Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission.

Genetically Encoded FRET Biosensors to Illuminate Compartmentalised GPCR Signalling (2017)
Journal Article

Genetically encoded Förster resonance energy transfer (FRET) biosensors have been instrumental to our understanding of how intracellular signalling is organised and regulated within cells. In the last decade, the toolbox, dynamic range and applicatio... Read More about Genetically Encoded FRET Biosensors to Illuminate Compartmentalised GPCR Signalling.

Ticks from diverse genera encode chemokine-inhibitory evasin proteins (2017)
Journal Article

To prolong residence on their hosts, ticks secrete many salivary factors that target host defense molecules. In particular, the tick Rhipicephalus sanguineus has been shown to produce three salivary glycoproteins named “evasins,” which bind to host c... Read More about Ticks from diverse genera encode chemokine-inhibitory evasin proteins.