Polyamine Conjugation as a Promising Strategy To Target Amyloid Aggregation in the Framework of Alzheimer's Disease(518 views) Simoni E, Caporaso R, Bergamini C, Fiori J, Fato R, Miszta P, Filipek S, Caraci F, Giuffrida ML, Andrisano V, Minarini A, Bartolini M, Rosini M
Acs Med Chem Lett (ISSN: 1948-5875, 1948-5875linking), 2016 Sep 26; 7(12): 1145-1150.
Keywords: Alzheimer, S Disease, Amyloid, Mitochondria, Polyamines,
Affiliations: *** IBB - CNR ***
Department of Pharmacy & Biotechnology, Alma Mater Studiorum-University of Bologna , Via Belmeloro 6, 40126 Bologna, Italy., Faculty of Chemistry, Biological & Chemical Research Centre University of Warsaw , Pasteura 1, 02093 Warsaw, Poland., IRCCS Associazione Oasi Maria S.S., Institute for Research on Mental Retardation and Brain Aging, Via Conte Ruggero 73, 94018 Troina, Enna, Italy; Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125 Catania, Italy., Institute of Biostructure and Bioimaging, National Research Council (CNR) , Via P. Gaifami 18, 95126 Catania, Italy., Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna , Corso D'Augusto 237, 47921 Rimini, Italy.,
References: Not available.
Polyamine Conjugation as a Promising Strategy To Target Amyloid Aggregation in the Framework of Alzheimer's Disease
Spermine conjugates 2-6, 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 2, which displayed effective antiaggregating activity and neuroprotective effects against Abeta-induced toxicity. Notably, a key functional role for the polyamine motif in Abeta 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 Abeta toxicity.
Polyamine Conjugation as a Promising Strategy To Target Amyloid Aggregation in the Framework of Alzheimer's Disease
Ciccarelli M, Sorriento D, Coscioni E, Iaccarino G, Santulli G * Adrenergic Receptors(329 views) Endocrinol Of The Heart In Health And Dis (ISSN: 9780-1280311249780128031117), 2016; N/D: 285-315. Impact Factor:0 ViewExport to BibTeXExport to EndNote