Effects of multi-kinase inhibitors on the activity of cytochrome P450 2J2.
CYP2J2
Ki
epoxyeicosatrienoic acid
inhibition
multi-kinase inhibitor
Journal
Xenobiotica; the fate of foreign compounds in biological systems
ISSN: 1366-5928
Titre abrégé: Xenobiotica
Pays: England
ID NLM: 1306665
Informations de publication
Date de publication:
Jul 2022
Jul 2022
Historique:
pubmed:
18
10
2022
medline:
15
12
2022
entrez:
17
10
2022
Statut:
ppublish
Résumé
1. Cytochrome P450 2J2 (CYP2J2) shows high expression in extrahepatic tissues, including the heart and kidney and in tumours. Inhibition of CYP2J2 has attracted attention for cancer treatment because it metabolises arachidonic acid (AA) to epoxyeicosatrienoic acid (EET), which inhibits apoptosis and promotes tumour growth. Multi-kinase inhibitor (MKI) is a molecular-targeted drug with antitumor activities. This study aimed to clarify the inhibitory effects of MKIs on CYP2J2 activity. We also investigated whether MKIs affected CYP2J2-catalysed EET formation from AA.2. Twenty MKIs showed different inhibitory potencies against astemizole
Identifiants
pubmed: 36251932
doi: 10.1080/00498254.2022.2137068
doi:
Substances chimiques
Cytochrome P-450 Enzyme System
9035-51-2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM