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Cited by 437Receptor Mechanisms and SignalingNeuroscience and Neuropharmacology ResearchNicotinic Acetylcholine Receptors Study

Muscarinic acetylcholine receptors: novel opportunities for drug development

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Kruse, Andrew C., Kobilka, Brian K., Gautam, Dinesh, Sexton, Patrick M., Christopoulos, Arthur, Wess, Jürgen·2014·Nature Reviews Drug Discovery
DOI 10.1038/nrd4295PMC PMC5818261
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Abstract

The muscarinic acetylcholine receptors are a subfamily of G protein-coupled receptors that regulate numerous fundamental functions of the central and peripheral nervous system. The past few years have witnessed unprecedented new insights into muscarinic receptor physiology, pharmacology and structure. These advances include the first structural views of muscarinic receptors in both inactive and active conformations, as well as a better understanding of the molecular underpinnings of muscarinic receptor regulation by allosteric modulators. These recent findings should facilitate the development of new muscarinic receptor subtype-selective ligands that could prove to be useful for the treatment of many severe pathophysiological conditions.

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Authors
Kruse, A. C., Kobilka, B. K., Gautam, D., Sexton, P. M., Christopoulos, A., & Wess, J.
Affiliations
  • Harvard University (US)
  • Stanford Medicine (US)
  • National Institutes of Health (US)
  • Monash University (AU)
Corresponding author
Wess, Jürgen
ORCID
Venue
Nature Reviews Drug Discovery
Publisher
Springer Science and Business Media LLC
Published
2014-06-06
Volume
13
Issue
7
Pages
549-560
ISSN
  • 1474-1776 (ISSN-L)
  • 1474-1784
DOI
10.1038/nrd4295
PMC
PMC5818261
OpenAlex
W2083180327
Cited by
437
References
5
Citations by year
2026: 28 · 2025: 33 · 2024: 37 · 2023: 39 · 2022: 35 · 2021: 37 · 2020: 38 · 2019: 36 · 2018: 36 · 2017: 39 · 2016: 37 · 2015: 29 · 2014: 11
FWCI
3.70
Type
journal article
Language
en
Open access
Licence
Locations
  • Nature Reviews Drug Discovery (publishedVersion)
  • PubMed (publishedVersion)
  • Europe PMC (PubMed Central) (acceptedVersion)
  • PubMed Central (acceptedVersion)
Funders
  • National Science Foundation (1223785)
  • National Institutes of Health
  • Medical Research Council
  • National Health and Medical Research Council (1055134)
  • National Institute of General Medical Sciences (U19GM106990)
  • National Institute of Diabetes and Digestive and Kidney Diseases
  • Division of Chemistry
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Keywords
muscarinic receptors, G protein-coupled receptors, allosteric modulators, subtype-selective ligands, Alzheimer's disease, type 2 diabetes
MeSH terms
Allosteric Regulation, Animals, Central Nervous System Diseases, Diabetes Mellitus, Type 2, Humans, Neoplasms, Receptors, Muscarinic, Muscarinic Agonists, Muscarinic Antagonists

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