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Kinetics are crucial when targeting copper ions to fight Alzheimer's disease: an illustration with azamacrocyclic ligands

Abstract : 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 ones 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.
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https://hal.univ-brest.fr/hal-01764900
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Submitted on : Monday, April 30, 2018 - 5:37:33 PM
Last modification on : Thursday, November 19, 2020 - 7:28:06 PM
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Amandine Conte-Daban, Maryline Beyler, Raphaël Tripier, Christelle Hureau. Kinetics are crucial when targeting copper ions to fight Alzheimer's disease: an illustration with azamacrocyclic ligands. Chemistry - A European Journal, Wiley-VCH Verlag, 2018, 24 (33), pp.8447-8452. ⟨10.1002/chem.201801520⟩. ⟨hal-01764900⟩

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