Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction.
Amino Acid Sequence
Binding Sites
Cell Line, Tumor
Cell Membrane Permeability
/ drug effects
Drug Design
Humans
Kelch-Like ECH-Associated Protein 1
/ antagonists & inhibitors
Molecular Dynamics Simulation
NF-E2-Related Factor 2
/ antagonists & inhibitors
Peptides
/ chemistry
Peptides, Cyclic
/ chemistry
Protein Binding
Structure-Activity Relationship
KEAP1/NRF2
PPI
Peptide Inhibitors
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 11 2020
01 11 2020
Historique:
received:
26
06
2020
revised:
20
08
2020
accepted:
21
08
2020
pubmed:
17
10
2020
medline:
22
6
2021
entrez:
16
10
2020
Statut:
ppublish
Résumé
Inhibition of KEAP1-NRF2 protein-protein interaction is considered a promising strategy to selectively and effectively activate NRF2, a transcription factor which is involved in several pathologies such as Huntington's disease (HD). A library of linear peptides based on the NRF2-binding motifs was generated on the nonapeptide lead Ac-LDEETGEFL-NH
Identifiants
pubmed: 33065433
pii: S0968-0896(20)30568-X
doi: 10.1016/j.bmc.2020.115738
pii:
doi:
Substances chimiques
Kelch-Like ECH-Associated Protein 1
0
NF-E2-Related Factor 2
0
Peptides
0
Peptides, Cyclic
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115738Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.