A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes

Autor: Mai, Quynh N., Shenoy, Priyank, Quach, Tim, Retamal, Jeffri S., Gondin, Arisbel B., Yeatman, Holly R., Aurelio, Luigi, Conner, Joshua W., Poole, Daniel P., Canals, Meritxell, Nowell, Cameron J., Graham, Bim, Davis, Thomas P., Briddon, Stephen J., Hill, Stephen J., Porter, Christopher J.H., Bunnett, Nigel W., Halls, Michelle L., Veldhuis, Nicholas A.

G-protein-coupled receptors (GPCRs) are traditionally known for signaling at the plasma membrane, but they can also signal from endosomes after internalization to control important pathophysiological processes. In spinal neurons, sustained endosomal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=core_ac_uk__::77698867f198c0456930778caa6598a0

Fluorogens: Generating Receptor-Specific Turn-On Fluorescence.

Autor: Conner, Joshua W.¹ josh.conner@monash.edu

Publikováno v: Australian Journal of Chemistry. 2018, Vol. 71 Issue 2/3, p197-199. 3p.

A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes.

Autor: Mai QN; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Medicinal Chemistry Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Shenoy P; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Quach T; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Retamal JS; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Gondin AB; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Yeatman HR; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Aurelio L; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Medicinal Chemistry Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Conner JW; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Medicinal Chemistry Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Poole DP; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Canals M; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, The University of Nottingham Medical School, Nottingham, UK; Centre of Membrane Proteins and Receptors, Universities of Birmingham and Nottingham, the Midlands, UK., Nowell CJ; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Graham B; Medicinal Chemistry Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Davis TP; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Institute for Bioengineering and Nanotechnology, University of Queensland, Brisbane, Queensland, Australia., Briddon SJ; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, The University of Nottingham Medical School, Nottingham, UK; Centre of Membrane Proteins and Receptors, Universities of Birmingham and Nottingham, the Midlands, UK., Hill SJ; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, The University of Nottingham Medical School, Nottingham, UK; Centre of Membrane Proteins and Receptors, Universities of Birmingham and Nottingham, the Midlands, UK., Porter CJH; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Bunnett NW; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Department of Pharmacology and Therapeutics, The University of Melbourne, Parkville, Victoria, Australia; Department of Molecular Pathobiology, New York University College of Dentistry, New York, New York, USA. Electronic address: nwb2@nyu.edu., Halls ML; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia. Electronic address: michelle.halls@monash.edu., Veldhuis NA; Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Drug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia. Electronic address: nicholas.veldhuis@monash.edu.

Publikováno v: The Journal of biological chemistry [J Biol Chem] 2021 Jan-Jun; Vol. 296, pp. 100345. Date of Electronic Publication: 2021 Jan 28.