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A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases.


ABSTRACT: (E)-6-Methyl-4'-amino-2-styrylquinoline (3) is a small molecule with the proper features to potentially diagnose, deliver therapy and monitor response to therapy in protein misfolding diseases. These features include compound fluorescent emission in the NIR region and its ability to interact with both A? and prion fibrils, staining them with high selectivity. Styrylquinoline 3 also inhibits A? self-aggregation in vitro and prion replication in the submicromolar range in a cellular context. Furthermore, it is not toxic and is able to cross the blood brain barrier in vitro (PAMPA test).

SUBMITTER: Staderini M 

PROVIDER: S-EPMC4027132 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases.

Staderini Matteo M   Aulić Suzana S   Bartolini Manuela M   Tran Hoang Ngoc Ai HN   González-Ruiz Víctor V   Pérez Daniel I DI   Cabezas Nieves N   Martínez Ana A   Martín M Antonia MA   Andrisano Vincenza V   Legname Giuseppe G   Menéndez J Carlos JC   Bolognesi Maria Laura ML  

ACS medicinal chemistry letters 20121228 2


(E)-6-Methyl-4'-amino-2-styrylquinoline (3) is a small molecule with the proper features to potentially diagnose, deliver therapy and monitor response to therapy in protein misfolding diseases. These features include compound fluorescent emission in the NIR region and its ability to interact with both Aβ and prion fibrils, staining them with high selectivity. Styrylquinoline 3 also inhibits Aβ self-aggregation in vitro and prion replication in the submicromolar range in a cellular context. Furth  ...[more]

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