Proflavine derivatives as fluorescent imaging agents of amyloid deposits
Autor: | M. Sallanon, Andrew B. Mahon, Martine Demeunynck, Fatima Oukhatar, Andrew C. Try, Sabine Chierici, Michel Dubois-Dauphin, Dominique Garin, Frank M. LaFerla |
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Přispěvatelé: | Radiopharmaceutiques Biocliniques, Université Joseph Fourier - Grenoble 1 (UJF)-Institut National de la Santé et de la Recherche Médicale (INSERM), Département de Chimie Moléculaire - Ingéniérie et Intéractions BioMoléculaires (DCM - I2BM), Département de Chimie Moléculaire (DCM), Université Joseph Fourier - Grenoble 1 (UJF)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Joseph Fourier - Grenoble 1 (UJF)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Macquarie University, University of Geneva [Switzerland], University of California [Irvine] (UCI), University of California |
Rok vydání: | 2011 |
Předmět: |
Amyloid
Ratón Clinical Biochemistry Pharmaceutical Science Hippocampus Mice Transgenic Plaque Amyloid Biochemistry 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine Alzheimer Disease Drug Discovery [CHIM]Chemical Sciences Animals Molecular Biology Proflavine ComputingMilieux_MISCELLANEOUS 030304 developmental biology Fluorescent Dyes chemistry.chemical_classification 0303 health sciences Amyloid beta-Peptides Organic Chemistry Fluorescence In vitro Peptide Fragments 3. Good health Staining Disease Models Animal chemistry Microscopy Fluorescence Molecular Medicine Glycoprotein 030217 neurology & neurosurgery |
Zdroj: | Bioorganic and Medicinal Chemistry Letters Bioorganic and Medicinal Chemistry Letters, Elsevier, 2011, 21 (8), pp.2203-2206. ⟨10.1016/j.bmcl.2011.03.010⟩ |
ISSN: | 1464-3405 0960-894X |
DOI: | 10.1016/j.bmcl.2011.03.010⟩ |
Popis: | A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23 months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ 40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections. |
Databáze: | OpenAIRE |
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