Chemical Modification of Phage-Displayed Helix-Loop-Helix Peptides to Construct Kinase-Focused Libraries.
bivalent inhibitors
modality
peptide library
phage display
protein kinases
Journal
Chembiochem : a European journal of chemical biology
ISSN: 1439-7633
Titre abrégé: Chembiochem
Pays: Germany
ID NLM: 100937360
Informations de publication
Date de publication:
10 12 2021
10 12 2021
Historique:
revised:
01
10
2021
received:
27
08
2021
pubmed:
5
10
2021
medline:
26
2
2022
entrez:
4
10
2021
Statut:
ppublish
Résumé
Conformationally constrained peptides hold promise as molecular tools in chemical biology and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chemically modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip-3 retained the α-helical structure and bound to AurA with a K
Identifiants
pubmed: 34605137
doi: 10.1002/cbic.202100450
pmc: PMC9297947
doi:
Substances chimiques
Peptide Library
0
Peptides
0
Protein Kinase Inhibitors
0
AURKA protein, human
EC 2.7.11.1
Aurora Kinase A
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
3406-3409Subventions
Organisme : JSPS KAKENHI
ID : 26870503
Informations de copyright
© 2021 The Authors. ChemBioChem published by Wiley-VCH GmbH.
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