Human Plasma In-Cell Western Assays-An In vitro Predictor for In vivo Pharmacology in Oncology Drug Discovery.
drug discovery
in vivo potency
in-cell Western
plasma protein binding
Journal
Current protocols
ISSN: 2691-1299
Titre abrégé: Curr Protoc
Pays: United States
ID NLM: 101773894
Informations de publication
Date de publication:
Feb 2021
Feb 2021
Historique:
entrez:
15
2
2021
pubmed:
16
2
2021
medline:
22
6
2021
Statut:
ppublish
Résumé
Evaluation of in vivo potencies plays an important role in drug discovery. Traditionally, the cellular activity and percent of plasma protein binding of a test agent are evaluated separately, with the plasma protein binding-adjusted cellular potency computation used to estimate in vivo potency. This process is costly, takes weeks to complete, and is increasingly unreliable for compounds that bind extensively to plasma proteins. Described in this article is a simple, high-throughput human plasma in-cell Western (ICW) assay that directly incorporates plasma protein binding into a cellular pharmacodynamic assay to provide a rapid and accurate estimate of in vivo potencies. The assay is versatile and can be readily employed for various targets that require short treatment periods for displaying maximal biological responses. © 2021 Wiley Periodicals LLC. Basic Protocol: Concentration-dependent human plasma ICW assay to determine test compound IC
Substances chimiques
Blood Proteins
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
e51Commentaires et corrections
Type : ErratumIn
Type : ErratumIn
Informations de copyright
© 2021 Wiley Periodicals LLC.
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