Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists-Reference-Cited by-同舟云学术

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

Published:2020-03-31 Issue:625 Volume:13 Page:
ISSN:1945-0877
Container-title:Science Signaling
language:en
Short-container-title:Sci. Signal.

Author:

Gillis Alexander¹^ORCID,Gondin Arisbel B.²^ORCID,Kliewer Andrea³^ORCID,Sanchez Julie²⁴⁵^ORCID,Lim Herman D.²,Alamein Claudia¹^ORCID,Manandhar Preeti⁶^ORCID,Santiago Marina⁶^ORCID,Fritzwanker Sebastian³,Schmiedel Frank³,Katte Timothy A.⁷^ORCID,Reekie Tristan⁷^ORCID,Grimsey Natasha L.⁸^ORCID,Kassiou Michael⁷^ORCID,Kellam Barrie⁹^ORCID,Krasel Cornelius¹⁰^ORCID,Halls Michelle L.²^ORCID,Connor Mark⁶^ORCID,Lane J. Robert⁴⁵^ORCID,Schulz Stefan³^ORCID,Christie Macdonald J.¹^ORCID,Canals Meritxell²⁴⁵^ORCID

Affiliation:

1. Discipline of Pharmacology, School of Medical Sciences, University of Sydney, NSW 2006, Australia.

2. Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, VIC 3052, Australia.

3. Institute of Pharmacology and Toxicology, Jena University Hospital, Friedrich-Schiller-University, 07747 Jena, Germany.

4. Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen’s Medical Centre, University of Nottingham, Nottingham, UK.

5. Centre of Membrane Proteins and Receptors, Universities of Birmingham and Nottingham, Midlands, UK.

6. Department of Biomedical Sciences, Macquarie University, NSW 2109, Australia.

7. School of Chemistry, University of Sydney, NSW 2006, Australia.

8. Department of Pharmacology and Clinical Pharmacology, School of Medical Sciences, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand.

9. School of Pharmacy, Centre for Biomolecular Sciences, University of Nottingham, Nottingham NG7 2RD, UK.

10. Department of Pharmacology and Toxicology, Philipps-University Marburg, D-35043 Marburg, Germany.

Abstract

Low intrinsic efficacy can explain the reduced side effects of apparently biased μ-opioid receptor agonists.

Funder

National Health and Medical Research Council

Auckland Medical Research Foundation

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Cell Biology,Molecular Biology,Biochemistry

Reference72 articles.

1. Regulation of µ-Opioid Receptors: Desensitization, Phosphorylation, Internalization, and Tolerance

2. Enhanced Morphine Analgesia in Mice Lacking β-Arrestin 2

3. Morphine Side Effects in β-Arrestin 2 Knockout Mice

4. Biased ligands at G-protein-coupled receptors: promise and progress

5. Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects

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