Unexpected CK2β-antagonistic functionality of bisubstrate inhibitors targeting protein kinase CK2.
Benzimidazoles
/ chemistry
Casein Kinase II
/ antagonists & inhibitors
Catalytic Domain
/ drug effects
Crystallography, X-Ray
Halogenation
Humans
Molecular Docking Simulation
Protein Kinase Inhibitors
/ chemistry
Protein Multimerization
/ drug effects
Protein Structure, Quaternary
/ drug effects
Protein Subunits
/ antagonists & inhibitors
Bisubstrate inhibitor
CK2β antagonists
Capillary electrophoresis-based kinase assay
Fluorescence anisotropy assay
Microscale thermophoresis
Protein kinase CK2
Protein/protein interaction
X-ray crystallography
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
03 2020
03 2020
Historique:
received:
15
10
2019
revised:
11
12
2019
accepted:
20
01
2020
pubmed:
15
2
2020
medline:
27
2
2021
entrez:
15
2
2020
Statut:
ppublish
Résumé
Protein kinase CK2, a heterotetrameric holoenzyme composed of two catalytic chains (CK2α) attached to a homodimer of regulatory subunits (CK2β), is a target for drug development for cancer therapy. Here, we describe the tetraiodobenzimidazole derivative ARC-3140, a bisubstrate inhibitor addressing the ATP site and the substrate-binding site of CK2 with extraordinary affinity (K
Identifiants
pubmed: 32058103
pii: S0045-2068(19)31727-4
doi: 10.1016/j.bioorg.2020.103608
pii:
doi:
Substances chimiques
Benzimidazoles
0
Protein Kinase Inhibitors
0
Protein Subunits
0
CSNK2A1 protein, human
EC 2.7.11.1
Casein Kinase II
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
103608Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that there is no conflict of interest.