Synthesis and Assessment of Novel Probes for Imaging Tau Pathology in Transgenic Mouse and Rat Models.


Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
02 06 2021
Historique:
pubmed: 11 3 2021
medline: 22 6 2021
entrez: 10 3 2021
Statut: ppublish

Résumé

Aggregated tau protein is a core pathology present in several neurodegenerative diseases. Therefore, the development and application of positron emission tomography (PET) imaging radiotracers that selectively bind to aggregated tau in fibril form is of importance in furthering the understanding of these disorders. While radiotracers used in human PET studies offer invaluable insight, radiotracers that are also capable of visualizing tau fibrils in animal models are important tools for translational research into these diseases. Herein, we report the synthesis and characterization of a novel library of compounds based on the phenyl/pyridinylbutadienylbenzothiazoles/benzothiazolium (PBB3) backbone developed for this application. From this library, we selected the compound LM229, which binds to recombinant tau fibrils with high affinity (

Identifiants

pubmed: 33689290
doi: 10.1021/acschemneuro.0c00790
pmc: PMC8176454
doi:

Substances chimiques

tau Proteins 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1885-1893

Subventions

Organisme : Medical Research Council
ID : MC_U105184291
Pays : United Kingdom
Organisme : Medical Research Council
ID : MR/K02308X/1
Pays : United Kingdom

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Auteurs

Lindsay McMurray (L)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Jennifer A Macdonald (JA)

MRC Laboratory of Molecular Biology, Cambridge CB2 0QH, United Kingdom.

Nisha Kuzhuppilly Ramakrishnan (NK)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Yanyan Zhao (Y)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

David W Williamson (DW)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Ole Tietz (O)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Xiaoyun Zhou (X)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Steven Kealey (S)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Steven G Fagan (SG)

Department of Clinical Neurosciences, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Tomáš Smolek (T)

Axon Neuroscience R&D Services SE, Bratislava, Slovak Republic 811 02.

Veronika Cubinkova (V)

Axon Neuroscience R&D Services SE, Bratislava, Slovak Republic 811 02.

Norbert Žilka (N)

Axon Neuroscience R&D Services SE, Bratislava, Slovak Republic 811 02.

Maria Grazia Spillantini (MG)

Department of Clinical Neurosciences, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Aviva M Tolkovsky (AM)

Department of Clinical Neurosciences, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

Michel Goedert (M)

MRC Laboratory of Molecular Biology, Cambridge CB2 0QH, United Kingdom.

Franklin I Aigbirhio (FI)

Molecular Imaging Chemistry Laboratory, Wolfson Brain Imaging Centre, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.
Department of Clinical Neurosciences, University of Cambridge, Cambridge CB2 0QQ, United Kingdom.

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Classifications MeSH