Assessing the Inhibitory Potential of Kinase Inhibitors In Vitro: Major Pitfalls and Suggestions for Improving Comparability of Data Using CK1 Inhibitors as an Example.
CK1
IC50
Ki
inhibitor constant
protein kinase
small molecule inhibitor
standardization
workflow
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
12 Aug 2021
12 Aug 2021
Historique:
received:
25
06
2021
revised:
06
08
2021
accepted:
09
08
2021
entrez:
27
8
2021
pubmed:
28
8
2021
medline:
9
9
2021
Statut:
epublish
Résumé
Phosphorylation events catalyzed by protein kinases represent one of the most prevalent as well as important regulatory posttranslational modifications, and dysregulation of protein kinases is associated with the pathogenesis of different diseases. Therefore, interest in developing potent small molecule kinase inhibitors has increased enormously within the last two decades. A critical step in the development of new inhibitors is cell-free in vitro testing with the intention to determine comparable parameters like the commonly used IC
Identifiants
pubmed: 34443486
pii: molecules26164898
doi: 10.3390/molecules26164898
pmc: PMC8401859
pii:
doi:
Substances chimiques
Protein Kinase Inhibitors
0
Casein Kinase I
EC 2.7.11.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Else Kröner-Fresenius-Stiftung
ID : 2017_A142
Organisme : Deutsche Forschungsgemeinschaft
ID : KN356/9-1
Organisme : Deutsche Forschungsgemeinschaft
ID : PE1605/34-1
Organisme : Deutsche Forschungsgemeinschaft
ID : GSC270
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