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Kinetics Are Crucial When Targeting Copper Ions to Fight Alzheimer's Disease: An Illustration with Azamacrocyclic Ligands
Author(s) -
ConteDaban Amandine,
Beyler Maryline,
Tripier Raphaël,
Hureau Christelle
Publication year - 2018
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201801520
Subject(s) - context (archaeology) , copper , kinetics , selectivity , chemistry , combinatorial chemistry , drug , pharmacology , biochemistry , biology , organic chemistry , physics , paleontology , quantum mechanics , catalysis
Targeting copper ions to either remove or redistribute them is currently viewed as a possible therapeutic strategy in the context of Alzheimer's disease (AD). Thermodynamic parameters, as for instance the copper(II) affinity of the drug candidate or the copper(II) over zinc(II) selectivity, are considered in the design of the drug candidate. In contrast, kinetic factors have been overlooked despite their probable high importance. In the present article, we use a series of azamacrocyclic ligands to demonstrate that kinetic issues must be taken into account when designing copper‐targeting drug candidates in the context of AD.