Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gastrointestinal motility disorders

Autor: DiCello, Jesse J., Carbone, Simona Elisa, Saito, Ayame, Pham, Vi, Szymaszkiewicz, Agata, Gondin, Arisbel B., Alvi, Sadia, Marique, Kiliana, Shenoy, Priyank, Veldhuis, Nicholas A., Fichna, Jakub, Canals, Meritxell, Christopoulos, Arthur, Valant, Celine, Poole, Daniel P.

Allosteric modulators (AMs) are molecules that can fine-tune signaling by G protein-coupled receptors (GPCRs). Although they are a promising therapeutic approach for treating a range of disorders, allosteric modulation of GPCRs in the context of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=core_ac_uk__::c64d33bbc5323d34bb2f432d7253f84b

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

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Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gastrointestinal motility disorders.

Autor: DiCello JJ; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Department of Physiology, Monash University Biomedicine Discovery Institute, Clayton, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia., Carbone SE; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia., Saito A; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Pham V; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Szymaszkiewicz A; Department of Biochemistry, Faculty of Medicine, Medical University of Lodz, Lodz, Poland., Gondin AB; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia., Alvi S; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Marique K; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Shenoy P; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia., Veldhuis NA; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia., Fichna J; Department of Biochemistry, Faculty of Medicine, Medical University of Lodz, Lodz, Poland., Canals M; Division of Physiology, Pharmacology and Neuroscience, Queen's Medical Centre, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.; Centre of Membrane Proteins and Receptors, Universities of Birmingham and Nottingham, The Midlands, United Kingdom., Christopoulos A; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Valant C; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia., Poole DP; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.; Australian Research Council Centre of Excellence in Convergent Bio-Nano Science and Technology, Parkville, Victoria, Australia.

Publikováno v: American journal of physiology. Gastrointestinal and liver physiology [Am J Physiol Gastrointest Liver Physiol] 2022 Jan 01; Vol. 322 (1), pp. G66-G78. Date of Electronic Publication: 2021 Nov 10.