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
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:
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