New Perspectives of CYP1B1 Inhibitors in the Light of Molecular Studies

Human cytochrome P450 1B1 (CYP1B1) is an extrahepatic heme-containing monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and endogenous substrates like melatonin, fatty acids, steroid hormones, and retinoids, which are involved in diverse critical cellular functions...

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Bibliographic Details
Published in:Processes 2021-05, Vol.9 (5), p.817
Main Authors: Mikstacka, Renata, Dutkiewicz, Zbigniew
Format: Article
Language:English
Subjects:
Antitumor agents
Binding sites
Breast cancer
Cancer
Cancer therapies
Carcinogenesis
Carcinogens
Cardiovascular diseases
Chemotherapy
Computer applications
Cytochrome
Cytochrome P450
Cytochromes P450
Cytotoxicity
DNA methylation
Drug metabolism
Drug resistance
Enzymes
Eye diseases
Fatty acids
Gene expression
Glaucoma
Heme
Homeostasis
Hormones
Hyperoxia
Hypertension
Melatonin
Metabolism
Metabolites
Molecular dynamics
Molecular interactions
Monooxygenase
Mutation
Oxidative metabolism
Oxidative stress
Pathogenesis
Retinoids
Steroid hormones
Substrate inhibition
Transcription factors
Tumor cells
Xenobiotics
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Summary:Human cytochrome P450 1B1 (CYP1B1) is an extrahepatic heme-containing monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and endogenous substrates like melatonin, fatty acids, steroid hormones, and retinoids, which are involved in diverse critical cellular functions. CYP1B1 plays an important role in the pathogenesis of cardiovascular diseases, hormone-related cancers and is responsible for anti-cancer drug resistance. Inhibition of CYP1B1 activity is considered as an approach in cancer chemoprevention and cancer chemotherapy. CYP1B1 can activate anti-cancer prodrugs in tumor cells which display overexpression of CYP1B1 in comparison to normal cells. CYP1B1 involvement in carcinogenesis and cancer progression encourages investigation of CYP1B1 interactions with its ligands: substrates and inhibitors. Computational methods, with a simulation of molecular dynamics (MD), allow the observation of molecular interactions at the binding site of CYP1B1, which are essential in relation to the enzyme’s functions.
ISSN:2227-9717
2227-9717
DOI:10.3390/pr9050817