Two Functions, One Molecule: A Metal‐Binding and a Targeting Moiety to Combat Alzheimer's Disease
Abstract
Merging pharmacophores: Aggregation of the peptide amyloid-β (Aβ) is responsible for the development of Alzheimer's disease. Metal ions bound to Aβ can promote aggregation and oxidative stress, and can thus have a detrimental effect. Disruption of these processes with chelators, as well as targeting these chelators towards Aβ aggregates is therefore a promising strategy.
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Two approaches have been pursued in BFC design: direct incorporation of metal-binding atom donors into the structural framework of an Aβ-interacting compound, and linking the metal-chelating and Aβ-binding molecular fragments.
“In this context, two approaches have been pursued in BFC design. 31,49–58 One strategy is based on the direct incorporation of metal-binding atom donors into the structural framework of an Aβ-interacting compoud (Scheme 1, approach A), and the other involves linking the metal-chelating and Aβ-binding molecular fragments (Scheme 1, approach B).”
From Bifunctional Compounds for Controlling Metal-Mediated Aggregation of the Aβ<sub>42</sub>Peptide (2012) · cites this paper as [55]
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- Authors
- Hureau, C., Sasaki, I., Gras, E., & Faller, P.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- Corresponding author
- Faller, Peter
- Venue
- ChemBioChem
- Publisher
- Wiley
- Published
- 2010-04-27
- Volume
- 11
- Issue
- 7
- Pages
- 950-953
- ISSN
- 1439-4227 (ISSN-L)
- 1439-7633
- OpenAlex
- W2100621472
- Cited by
- 49
- References
- 23
- Citations by year
- 2023: 2 · 2021: 2 · 2019: 1 · 2018: 4 · 2017: 1 · 2016: 2 · 2015: 5 · 2014: 6 · 2013: 3 · 2012: 10
- FWCI
- 5.63
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- ChemBioChem (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Agence Nationale de la Recherche
- Topics
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Physical Sciences › Chemistry › Spectroscopy › Molecular Sensors and Ion Detection
- Keywords
- Alzheimer's disease, amyloid-beta aggregation, metal ions, metal chelators, metal-binding peptides, targeting moieties, oxidative stress
- MeSH terms
- Alzheimer Disease, Chelating Agents, Metals, Amyloid beta-Peptides, Oxidative Stress, Amyloid Precursor Protein Secretases
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