Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
14 05 2020
14 05 2020
Historique:
pubmed:
18
4
2020
medline:
3
11
2020
entrez:
18
4
2020
Statut:
ppublish
Résumé
Mammary-tissue-restricted cytochrome P450 4Z1 (CYP4Z1) has garnered interest for its potential role in breast cancer progression. CYP4Z1-dependent metabolism of arachidonic acid preferentially generates 14,15-epoxyeicosatrienoic acid (14,15-EET), a metabolite known to influence cellular proliferation, migration, and angiogenesis. In this study, we developed time-dependent inhibitors of CYP4Z1 designed as fatty acid mimetics linked to the bioactivatable pharmacophore, 1-aminobenzotriazole (
Identifiants
pubmed: 32302132
doi: 10.1021/acs.jmedchem.0c00101
doi:
Substances chimiques
Cytochrome P-450 Enzyme Inhibitors
0
Fatty Acids
0
Triazoles
0
Arachidonic Acid
27YG812J1I
CYP4Z1 protein, human
EC 1.14.14.1
Cytochrome P450 Family 4
EC 1.14.14.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM