An easy-to-implement combinatorial approach involving an activity-based assay for the discovery of a peptidyl copper complex mimicking superoxide dismutase

A combinatorial approach using a one-bead-one-compound method and a screening based on a SOD-activity assay was set up for the discovery of an efficient peptidyl copper complex. The complex exhibited good stability constants, suitable redox potentials and excellent intrinsic activity. This complex w...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2020-01, Vol.56 (3), p.399-42
Hauptverfasser: Vincent, Amandine, Fores, Jennifer Rodon, Tauziet, Elodie, Quévrain, Elodie, Dancs, Ágnes, Conte-Daban, Amandine, Bernard, Anne-Sophie, Pelupessy, Philippe, Coulibaly, Koudedja, Seksik, Philippe, Hureau, Christelle, Selmeczi, Katalin, Policar, Clotilde, Delsuc, Nicolas
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container_end_page 42
container_issue 3
container_start_page 399
container_title Chemical communications (Cambridge, England)
container_volume 56
creator Vincent, Amandine
Fores, Jennifer Rodon
Tauziet, Elodie
Quévrain, Elodie
Dancs, Ágnes
Conte-Daban, Amandine
Bernard, Anne-Sophie
Pelupessy, Philippe
Coulibaly, Koudedja
Seksik, Philippe
Hureau, Christelle
Selmeczi, Katalin
Policar, Clotilde
Delsuc, Nicolas
description A combinatorial approach using a one-bead-one-compound method and a screening based on a SOD-activity assay was set up for the discovery of an efficient peptidyl copper complex. The complex exhibited good stability constants, suitable redox potentials and excellent intrinsic activity. This complex was further assayed in cells for its antioxidant properties and showed beneficial effects when cells were subjected to oxidative stress. A strategy combining combinatorial chemistry and an activity-based screening leads to the development of a peptidyl catalytic drug that reduces the oxidative stress in cellular models.
doi_str_mv 10.1039/c9cc07920c
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source MEDLINE; Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection
subjects Amino Acid Sequence
Antioxidants
Assaying
Biocompatible Materials - chemistry
Biocompatible Materials - metabolism
Biocompatible Materials - pharmacology
Chemical Sciences
Colon - cytology
Colon - drug effects
Colon - metabolism
Combinatorial analysis
Coordination chemistry
Coordination compounds
Copper
Copper - chemistry
Copper - metabolism
Copper compounds
HT29 Cells
Humans
Interleukin-8 - metabolism
Lipopolysaccharides - toxicity
Oxidation
Oxidative Stress - drug effects
Peptides - chemistry
Peptides - metabolism
Stability constants
Superoxide dismutase
Superoxide Dismutase - metabolism
title An easy-to-implement combinatorial approach involving an activity-based assay for the discovery of a peptidyl copper complex mimicking superoxide dismutase
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