(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. Furthermore, it is not toxic and is able to cross the blood brain barrier in vitro (PAMPA test).
A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases / Staderini, M; Aulić, S; Bartolini, M; Tran, Hna; GONZÁLEZ RUIZ, V; Pérez, Di; Cabezas, N; Martínez, A; Martín, Am; Andrisano, V; Legname, Giuseppe; Menéndez, Jc; Bolognesi, Ml. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 4:2(2012), pp. 225-229. [10.1021/ml3003605]
A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer’s and Prion Diseases
Legname, Giuseppe;
2012-01-01
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 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. Furthermore, it is not toxic and is able to cross the blood brain barrier in vitro (PAMPA test).| File | Dimensione | Formato | |
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