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Title: Kororamides, convolutamines, and indole derivatives as possible tau and dual specificity kinases inhibitors for Alzheimer's Disease
Author: Llorach Parés, Laura
Nonell Canals, Alfons
Sánchez Martínez, Melchor
Avila, Conxita
Keywords: Malaltia d'Alzheimer
Disseny de medicaments
Alzheimer's disease
Drug design
Issue Date: 16-Oct-2018
Publisher: MDPI
Abstract: Alzheimer's disease (AD) is becoming one of the most disturbing health and socioeconomic problems nowadays, as it is a neurodegenerative pathology with no treatment, which is expected to grow further due to population ageing. Actual treatments for AD produce only a modest amelioration of symptoms, although there is a constant ongoing research of new therapeutic strategies oriented to improve the amelioration of the symptoms, and even to completely cure the disease. A principal feature of AD is the presence of neurofibrillary tangles (NFT) induced by the aberrant phosphorylation of the microtubule-associated protein tau in the brains of affected individuals. Glycogen synthetase kinase-3 beta (GSK3β), casein kinase 1 delta (CK1δ), dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) and dual-specificity kinase cdc2-like kinase 1 (CLK1) have been identified as the principal proteins involved in this process. Due to this, the inhibition of these kinases has been proposed as a plausible therapeutic strategy to fight AD. In this study, we tested in silico the inhibitory activity of different marine natural compounds, as well as newly-designed molecules from some of them, over the mentioned protein kinases, finding some new possible inhibitors with potential therapeutic application.
Note: Reproducció del document publicat a:
It is part of: Marine Drugs, 2018, vol. 16, num. 10, p. 386
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ISSN: 1660-3397
Appears in Collections:Articles publicats en revistes (Biologia Evolutiva, Ecologia i Ciències Ambientals)

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