A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer鈥檚 and Prion Diseases

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• 作者：Matteo Staderini ; Suzana Auli膰 ; Manuela Bartolini ; Hoang Ngoc Ai Tran ; V铆ctor Gonz谩lez-Ruiz ; Daniel I. P茅rez ; Nieves Cabezas ; Ana Mart铆nez ; M. Antonia Mart铆n ; Vincenza Andrisano ; Giuseppe Legname ; J. Carlos Men茅ndez ; Maria Laura Bolognesi
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：February 14, 2013
• 年：2013
• 卷：4
• 期：2
• 页码：225-229
• 全文大小：287K
• 年卷期：v.4,no.2(February 14, 2013)
• ISSN：1948-5875

文摘

(E)-6-Methyl-4鈥?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尾 and prion fibrils, staining them with high selectivity. Styrylquinoline 3 also inhibits A尾 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).

Keywords:

Aggregation; protein misfolding diseases; amyloid; fibrillation inhibitors