Inhibition of human CYP1 enzymes by a classical inhibitor α-naphthoflavone and a novel inhibitor N-(3, 5-dichlorophenyl)cyclopropanecarboxamide: An in vitro and in silico study.
Amides
/ chemistry
Benzoflavones
/ chemistry
Binding Sites
Catalytic Domain
Coumarins
/ chemistry
Cyclopropanes
/ chemistry
Cytochrome P-450 CYP1A1
/ antagonists & inhibitors
Cytochrome P-450 CYP1A2
/ chemistry
Cytochrome P-450 CYP1B1
/ antagonists & inhibitors
Cytochrome P-450 Enzyme Inhibitors
/ chemistry
Cytochrome P450 Family 1
/ antagonists & inhibitors
Humans
Liver
/ enzymology
Molecular Dynamics Simulation
Oxidation-Reduction
CYP
N-(3,5-dichlorophenyl)cyclopropanecarboxamide
human
inhibition
mechanism
α-naphthoflavone
Journal
Chemical biology & drug design
ISSN: 1747-0285
Titre abrégé: Chem Biol Drug Des
Pays: England
ID NLM: 101262549
Informations de publication
Date de publication:
05 2020
05 2020
Historique:
received:
20
11
2019
revised:
08
01
2020
accepted:
25
01
2020
pubmed:
16
2
2020
medline:
13
5
2021
entrez:
16
2
2020
Statut:
ppublish
Résumé
Enzymes in the cytochrome P450 family 1 (CYP1) catalyze metabolic activation of procarcinogens and deactivation of certain anticancer drugs. Inhibition of these enzymes is a potential approach for cancer chemoprevention and treatment of CYP1-mediated drug resistance. We characterized inhibition of human CYP1A1, CYP1A2, and CYP1B1 enzymes by the novel inhibitor N-(3,5-dichlorophenyl)cyclopropanecarboxamide (DCPCC) and α-naphthoflavone (ANF). Depending on substrate, IC
Substances chimiques
Amides
0
Benzoflavones
0
Coumarins
0
Cyclopropanes
0
Cytochrome P-450 Enzyme Inhibitors
0
alpha-naphthoflavone
604-59-1
coumarin
A4VZ22K1WT
CYP1A2 protein, human
EC 1.14.14.1
CYP1B1 protein, human
EC 1.14.14.1
Cytochrome P-450 CYP1A1
EC 1.14.14.1
Cytochrome P-450 CYP1A2
EC 1.14.14.1
Cytochrome P-450 CYP1B1
EC 1.14.14.1
Cytochrome P450 Family 1
EC 1.14.14.1
cyclopropanecarboxamide
NA7A3S4MUT
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
520-533Informations de copyright
© 2020 John Wiley & Sons A/S.
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