ArticleThe Journal of biological chemistry
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.
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Article in The Journal of biological chemistry. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13citing papers in PubMed
1.5field-weighted citation impact, top 18% of its field
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- Structure-guided allosteric modulation of the delta opioid receptor.Nature communications · 2026Article
- Beyond neurotransmission: the roles of serotonylation in physiological and pathological processes.Cellular & molecular biology letters · 2026Review
- Mechanisms of Location Bias in G Protein-Coupled Receptors.Handbook of experimental pharmacology · 2026Review
- Pain Signaling by GPCRs and RTKs.Trends in pharmacological sciences · 2025Review
- GPCR kinases differentially modulate biased signaling downstream of CXCR3 depending on their subcellular localization.Science signaling · 2024Article
- Aprepitant Restores Corneal Sensitivity and Reduces Pain in DED.Translational vision science & technology · 2024Article
- Signalling of Adrenoceptors: Canonical Pathways and New Paradigms.Handbook of experimental pharmacology · 2024Review
- Location bias: A "Hidden Variable" in GPCR pharmacology.BioEssays : news and reviews in molecular, cellular and developmental biology · 2023Review
- Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Soluble cyclase-mediated nuclear cAMP synthesis is sufficient for cell proliferation.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- The effect of substance P and its common in vivo-formed metabolites on MRGPRX2 and human mast cell activation.Pharmacology research & perspectives · 2022Article
- Sustained endosomal release of a neurokinin-1 receptor antagonist from nanostars provides long-lasting relief of chronic pain.Biomaterials · 2022Article
- Engineering Nanoscale Drug Delivery Systems for Pain.Wiley interdisciplinary reviews. Nanomedicine and nanobiotechnologyReview
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
19 authors at 4 institutions in 3 countries.
Quynh N MaiDrug 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.
Priyank ShenoyDrug 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.
Tim QuachDrug Delivery, Disposition and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Jeffri S RetamalDrug 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.
Arisbel B GondinDrug 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.
Holly R YeatmanDrug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Luigi AurelioDrug 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.
Joshua W ConnerAustralian 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.
Daniel P PooleDrug 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.
Meritxell CanalsDivision 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.
Cameron J NowellDrug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Bim GrahamMedicinal Chemistry Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Thomas P DavisDrug 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.
Stephen J BriddonDivision 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.
Stephen J HillDivision 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.
Christopher J H PorterDrug 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.
Nigel W BunnettDrug 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.
Michelle L HallsDrug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia. Electronic address: michelle.halls@monash.edu.
Nicholas A VeldhuisDrug 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.
Australian Research Council · AUMonash University · AUUniversity of Nottingham · GBDiscovery Institute · US
Funding
Targeting Endosomal Receptors for Treatment of Chronic PainR01DE029951 · NIDCR · NEW YORK UNIVERSITY · PI BUNNETT, NIGEL W, SCHMIDT, BRIAN L · 2020 to 2024
$4.7MProtease/PAR2/TRPV4 Axis and Oral Cancer PainR01DE026806 · NIDCR · NEW YORK UNIVERSITY · PI BUNNETT, NIGEL W, SCHMIDT, BRIAN L · 2018 to 2022
$3.9MEndosomal Platforms for Signaling PainR01NS102722 · NINDS · NEW YORK UNIVERSITY · PI NIGEL W BUNNETT, Brian L Schmidt · 2017 to 2026
$3.4MTrafficking-Dependent Signaling of Pain by Protease-Activated ReceptorsR01DK118971 · NIDDK · NEW YORK UNIVERSITY · PI BUNNETT, NIGEL W, SCHMIDT, BRIAN L · 2018 to 2021
$3.2MMedical Research Council MR/N020081/1NIDCR NIH HHS R01 DE026806NIDCR NIH HHS R01 DE029951NIDDK NIH HHS R01 DK118971NINDS NIH HHS R01 NS102722
Abstract
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 signaling of the neurokinin 1 receptor (NK
Indexed as
AnalgesicsAnimalsCell MembraneCholestanolEndosomesHEK293 CellsHumansMaleMiceMice, Inbred C57BLNeurokinin-1 Receptor AntagonistsPainPain ManagementSubstance PAnalgesicsCholestanolNeurokinin-1 Receptor AntagonistsspantideSubstance Pcell signalingdrug deliveryendosomeG-protein-coupled receptorlipid conjugationpaintachykinin
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.