Polyamine Conjugation As a Promising Strategy To Target Amyloid Aggregation in the Framework of Alzheimer's Disease

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2016 Dec 21

PMID 27994754

Citations 7

Authors

Elena Simoni

Roberta Caporaso

Christian Bergamini

Jessica Fiori

Romana Fato

Przemyslaw Miszta

Slawomir Filipek

Filippo Caraci

Maria Laura Giuffrida

Vincenza Andrisano

Anna Minarini

Manuela Bartolini

Michela Rosini

Affiliations

Soon will be listed here.

Abstract

Spermine conjugates -, carrying variously decorated 3,5-dibenzylidenepiperidin-4-one as bioactive motives, were designed to direct antiaggregating properties into mitochondria, using a polyamine functionality as the vehicle tool. The study confirmed mitochondrial import of the catechol derivative , which displayed effective antiaggregating activity and neuroprotective effects against Aβ-induced toxicity. Notably, a key functional role for the polyamine motif in Aβ molecular recognition was also unraveled. This experimental readout, which was supported by in silico studies, gives important new insight into the polyamine's action. Hence, we propose polyamine conjugation as a promising strategy for the development of neuroprotectant leads that may contribute to decipher the complex picture of Aβ toxicity.

Citing Articles

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