ArticleeLife2023
Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics.
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In one paragraph
Article in eLife, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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0cells of the map it votes in
22citing papers in PubMed
5.1field-weighted citation impact, top 4% of its field
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Who cites it
22 citing papers in PubMed, 33 citations in OpenAlex.
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- Cryo-EM reveals an extrahelical allosteric binding site at the MNature communications · 2025Article
- Downstream Signaling of Muscarinic MPharmacology research & perspectives · 2025Article
- Discovering Key Activation Hotspots in the MJournal of the American Chemical Society · 2025Article
- Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery.Nature reviews. Drug discovery · 2025Review
- A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Anti-carcinogenic effects of arecaidine but-2-ynyl ester tosylate on breast cancer: proliferation inhibition and activation of apoptosis.Molecular biology reports · 2025Article
- High-resolution cryo-EM using a common LaBScience advances · 2025Article
- A golden age of muscarinic acetylcholine receptor modulation in neurological diseases.Nature reviews. Drug discovery · 2024Review
- Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.Nature reviews. Drug discovery · 2024Review
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- Allo-targeting of the kinase domain: Insights from in silico studies and comparison with experiments.Current opinion in structural biology · 2024Review
- Deepening insights into cholinergic agents for intraocular pressure reduction: systems genetics, molecular modeling, andFrontiers in molecular biosciences · 2024Article
- Mechanistic Insights into Peptide Binding and Deactivation of an Adhesion G Protein-Coupled Receptor.Molecules (Basel, Switzerland) · 2023Article
- Article
- Design, synthesis and evaluation of novel 2-phenyl-3-(1H-pyrazol-4-yl)pyridine positive allosteric modulators for the MEuropean journal of medicinal chemistry · 2023Article
- Xanomeline displays concomitant orthosteric and allosteric binding modes at the MNature communications · 2023Article
- Decoding the mechanisms of allostery.eLife · 2023Article
Corrections and comments
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Authors and funding
24 authors at 6 institutions in 5 countries.
Ziva Vuckovic *Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Jinan Wang *Center for Computational Biology and Department of Molecular Biosciences, University of Kansas, Lawrence, United States.
Vi Pham *Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Jesse I Mobbs *Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Matthew J BelousoffDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Apurba BhattaraiCenter for Computational Biology and Department of Molecular Biosciences, University of Kansas, Lawrence, United States.
Wessel A C BurgerDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Geoff ThompsonDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Mahmuda YeasminDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Vindhya NawaratneDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Katie LeachDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Emma T van der WesthuizenDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.ORCID 0000-0001-9165-8526
Elham KhajehaliDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Yi-Lynn LiangDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Alisa GlukhovaDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Denise WoottenDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Craig W LindsleyDepartment of Pharmacology, Warren Center for Neuroscience Drug Discovery and Department of Chemistry, Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, United States.
Andrew TobinThe Centre for Translational Pharmacology, Advanced Research Centre (ARC), College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom.ORCID 0000-0002-1807-3123
Patrick SextonDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Radostin DanevGraduate School of Medicine, University of Tokyo, Tokyo, Japan.
Celine ValantDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Yinglong MiaoCenter for Computational Biology and Department of Molecular Biosciences, University of Kansas, Lawrence, United States.
Arthur ChristopoulosDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.ORCID 0000-0003-4442-3294
David M ThalDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.ORCID 0000-0002-0325-2524
Monash University · AUUniversity of Kansas · USDiscovery Centre · CAThe University of Tokyo · JPUniversity of Glasgow · GBVanderbilt University · US
Funding
Enhanced Sampling of G-Protein-Coupled Receptor-G Protein InteractionsR01GM132572 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI MIAO, YINGLONG · 2019 to 2023
$1.5MNIGMS NIH HHS R01 GM132572Wellcome Trust
Abstract
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR allosteric modulators remains limited. The M
Indexed as
Receptor, Muscarinic M4Receptors, MuscarinicAcetylcholineAllosteric RegulationAllosteric SiteCryoelectron MicroscopyHumansLigandsNicotinic AcidsPyridazinesThiophenes3-amino-5-chloro-6-methoxy-4-methyl-thieno(2,3-b)pyridine-2-carboxylic acid cyclopropylamide5-amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno(2,3-c)pyridazine-6-carboxamideAcetylcholineLigandsNicotinic AcidsPyridazinesReceptor, Muscarinic M4Receptors, MuscarinicThiophenesallosterybiochemistrychemical biologydrug discoverymolecular biophysicsmolecular dynamicsmolecular pharmacologymuscarinic acetylcholine receptorsnonestructural biology
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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.