ArticleJournal of medicinal chemistry2019
Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery.
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Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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25citing papers in PubMed
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Who cites it
25 citing papers in PubMed.
- Current Landscape of Glycogen Synthase Kinase-3β PET Tracers: Progress, Limitations, and Perspectives-A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Current progress in pathway-targeted therapeutics for Alzheimer's disease: mechanistic insights and windows of opportunity.Molecular and cellular biochemistry · 2026Review
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- Evaluation of [ACS chemical neuroscience · 2025Article
- Radiosynthesis and Evaluation ofACS pharmacology & translational science · 2025Article
- Inhibition of GSK3α,β rescues cognitive phenotypes in a preclinical mouse model of CTNNB1 syndrome.EMBO molecular medicine · 2024Article
- Recent advances in Alzheimer's disease: Mechanisms, clinical trials and new drug development strategies.Signal transduction and targeted therapy · 2024Review
- Synthesis and preliminary evaluation of novel PET probes for GSK-3 imaging.Scientific reports · 2024Article
- Recent Advances in Pyrimidine-Based Drugs.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Radiosynthesis and evaluation of a novelAmerican journal of nuclear medicine and molecular imaging · 2024Article
- Development and Optimization ofACS pharmacology & translational science · 2023Review
- In Vivo Imaging and Kinetic Modeling of Novel Glycogen Synthase Kinase-3 Radiotracers [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Review
- Differentiation of Human Induced Pluripotent Stem Cells into Cortical Neurons to Advance Precision Medicine.Methods in molecular biology (Clifton, N.J.) · 2022Article
- PET imaging of glycogen synthase kinase-3 in pancreatic cancer xenograft mouse models.American journal of nuclear medicine and molecular imaging · 2022Article
- Characterization of neuroinflammatory positron emission tomography biomarkers in chronic traumatic encephalopathy.Brain communications · 2022Article
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- NRM 2021 Abstract Booklet.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Article
- Positron Emission Tomography in Animal Models of Alzheimer's Disease Amyloidosis: Translational Implications.Pharmaceuticals (Basel, Switzerland) · 2021Review
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Authors and funding
27 authors.
Vadim Bernard-GauthierAzrieli Centre for Neuro-Radiochemistry, Research Imaging Centre , Centre for Addiction and Mental Health , Toronto , Ontario M5T 1R8 , Canada.
Andrew V MossineDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Ashley KnightAzrieli Centre for Neuro-Radiochemistry, Research Imaging Centre , Centre for Addiction and Mental Health , Toronto , Ontario M5T 1R8 , Canada.ORCID 0000-0003-2225-360X
Debasis PatnaikChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Wen-Ning ZhaoChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0002-5824-2032
Chialin ChengChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Hema S KrishnanDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital and Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Lucius L XuanChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Peter S ChindavongChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Surya A ReisChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Jinshan Michael ChenPfizer Worldwide Research and Development , Groton Laboratories , Eastern Point Road , Groton , Connecticut 06340 , United States.
Xia ShaoDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Jenelle StauffDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Janna ArteagaDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Phillip ShermanDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Nicolas SalemBiogen, Research and Early Development Imaging , Cambridge , Massachusetts 02142 , United States.
David BonsallInvicro , London W12 0NN , U.K.
Brenda AmaralBiogen, Research and Early Development Imaging , Cambridge , Massachusetts 02142 , United States.
Cassis VarlowAzrieli Centre for Neuro-Radiochemistry, Research Imaging Centre , Centre for Addiction and Mental Health , Toronto , Ontario M5T 1R8 , Canada.
Lisa WellsInvicro , London W12 0NN , U.K.
Laurent MartarelloBiogen, Research and Early Development Imaging , Cambridge , Massachusetts 02142 , United States.
Shil PatelEisai AiM Institute , Boston , Massachusetts 01810 , United States.
Steven H LiangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital and Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0003-1413-6315
Ravi G KurumbailPfizer Worldwide Research and Development , Groton Laboratories , Eastern Point Road , Groton , Connecticut 06340 , United States.
Stephen J HaggartyChemical Neurobiology Laboratory, Massachusetts General Hospital, Center for Genomic Medicine, Departments of Neurology & Psychiatry , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0002-7872-168X
Peter J H ScottDivision of Nuclear Medicine, Department of Radiology , The University of Michigan Medical School , Ann Arbor , Michigan 48109 , United States.
Neil VasdevAzrieli Centre for Neuro-Radiochemistry, Research Imaging Centre , Centre for Addiction and Mental Health , Toronto , Ontario M5T 1R8 , Canada.ORCID 0000-0002-2087-5125
Funding
Neuro-PET Radiotracer Discovery for Imaging Glycogen Synthase Kinase-3R01AG054473 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI VASDEV, NEIL · 2017 to 2020
$1.7MNIA NIH HHS R01 AG054473
Abstract
Using structure-guided design, several cell based assays, and microdosed positron emission tomography (PET) imaging, we identified a series of highly potent, selective, and brain-penetrant oxazole-4-carboxamide-based inhibitors of glycogen synthase kinase-3 (GSK-3). An isotopologue of our first-generation lead, [
Indexed as
Drug DiscoveryAnimalsBlood-Brain BarrierBrainCatalytic DomainGlycogen Synthase Kinase 3 betaHEK293 CellsHumansMiceModels, MolecularNeuroimagingOxazolesPositron-Emission TomographyProtein Kinase InhibitorsTriazolesGlycogen Synthase Kinase 3 betaOxazolesPF-04802367Protein Kinase InhibitorsTriazoles
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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.