Cytochrome P450 3A4 as a Drug Metabolizing Enzyme: the Role of Sensor System Modifications in Electocatalysis and Electroanalysis

2020 ◽  
Vol 14 (3) ◽  
pp. 252-259
Author(s):  
A. V. Kuzikov ◽  
T. V. Bulko ◽  
P. I. Koroleva ◽  
R. A. Masamrekh ◽  
S. S. Babkina ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Sensor System ◽  
Cytochrome P450 3A4 ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme

scholarly journals Cytochrome P450 3A4 and 2D6-Mediated Metabolism of Leisure and Medicinal Teas

2014 ◽  
Vol 17 (3) ◽  
pp. 294 ◽  
Author(s):  
Teresa W Tam ◽  
Rui Liu ◽  
Ammar Saleem ◽  
John Thor Arnason ◽  
Anthony Krantis ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Metabolism ◽  
Camellia Sinensis ◽  
Plant Material ◽  
Tea Plant ◽  
Cytochrome P450 3A4 ◽  
Aqueous Extracts ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme

PURPOSE: Thirty-five commercially available Camellia sinensis (black and green) and herbal leisure teas and an assortment of Traditional Chinese medicinal teas were randomly selected and examined for their potential to inhibit the drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4). The study was then extended to examine CYP2D6*1 and CYP2D6*10. METHODS: Microtiter fluorometric assays were utilized to examine the potential for the teas to inhibit CYP-mediated metabolism. Aqueous or alcoholic extracts of the dried tea plant material were examined. METHODS: Most of the black and green leisure teas generally inhibited CYP3A4 more than the Chinese medicinal teas. The medicinal Chinese teas were generally more inhibitory towards CYP3A4 compared to the CYP2D6 isozymes, and the aqueous extracts displayed more potency than the alcoholic extracts. CONCLUSIONS: Tea whether used for leisure or medicinal purposes has the potential to inhibit CYP3A4-mediated drug metabolism particularly black tea.This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Structural Insights into the Interaction of Cytochrome P450 3A4 with Suicide Substrates: Mibefradil, Azamulin and 6′,7′-Dihydroxybergamottin

2019 ◽  
Vol 20 (17) ◽  
pp. 4245 ◽  
Author(s):  
Irina F. Sevrioukova
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 3A4 ◽  
Drug Metabolizing Enzyme ◽  
Human Cytochrome ◽  
Suicide Substrate ◽  
Metabolizing Enzyme ◽  
Structural Insights ◽  
Suicide Mechanism ◽  
Important Drug ◽  
Suicide Substrates

Human cytochrome P450 3A4 (CYP3A4) is the most important drug-metabolizing enzyme. Some drugs and natural compounds can act as suicide (mechanism-based) inactivators of CYP3A4, leading to unanticipated drug-drug interactions, toxicity and therapeutic failures. Despite significant clinical and toxicological implications, the mechanism-based inactivation remains incompletely understood. This study provides the first direct insights into the interaction of CYP3A4 with three suicide substrates: mibefradil, an antihypertensive drug quickly withdrawn from the market; a semi-synthetic antibiotic azamulin; and a natural furanocoumarin, 6′,7′-dihydroxybergamottin. Novel structural findings help better understand the suicide substrate binding and inhibitory mechanism, and can be used to improve the predictability of the binding ability, metabolic sites and inhibitory/inactivation potential of newly developed drugs and other chemicals relevant to public health.

scholarly journals Estimation of polymorphisms in the drug-metabolizing enzyme, cytochrome P450 2C19 gene in six major ethnicities of Pakistan

Bioengineered ◽  
2021 ◽  
Vol 12 (1) ◽  
pp. 4442-4451
Author(s):  
Sagheer Ahmed ◽  
Saima Gul ◽  
Muhammad Akhlaq ◽  
Abrar Hussain ◽  
Sidrah Tariq Khan ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Metabolizing Enzyme ◽  
Cytochrome P450 2C19 ◽  
Metabolizing Enzyme

scholarly journals Role of Cytochrome P450 3A4 and 1A2 Phenotyping in Patients with Advanced Non-small-Cell Lung Cancer Receiving Erlotinib Treatment

2017 ◽  
Vol 121 (4) ◽  
pp. 309-315 ◽  
Author(s):  
Zinnia P. Parra-Guillen ◽  
Peter B. Berger ◽  
Manuel Haschke ◽  
Massimiliano Donzelli ◽  
Daria Winogradova ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cytochrome P450 ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Cytochrome P450 3A4 ◽  
Small Cell Lung

Assessing Home Health Care Pharmacists' Knowledge of Cytochrome P450 Pharmacogenetics

2002 ◽  
Vol 18 (5) ◽  
pp. 248-253 ◽  
Author(s):  
Janyce F Rogers ◽  
Robert S Kidd
Keyword(s):  
Cytochrome P450 ◽  
Home Health Care ◽  
Formal Education ◽  
Care Facility ◽  
Cross Sectional Study ◽  
Cross Sectional ◽  
Web Based ◽  
Cytochrome P450 Activity ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme

Objective: Genetic code governs cytochrome P450 activity as a consequence, it may influence an individual's response to medications metabolized by these enzymes. Pharmacists have a prominent role in providing education concerning adverse drug reactions and variability in drug response. This investigation assessed the knowledge of a group of pharmacists regarding cytochrome P450 pharmacogenetics. Methods: This observational, cross-sectional study presented a Web–based questionnaire available for completion by pharmacists contacted via E-mail. Fifty-two pharmacists involved with a nationwide home-care facility participated in the study on a volunteer basis. The main outcome measure was percentage score on a 10-question examination. Results: Fifty-two of 171 contacted pharmacists participated in the study, yielding a response rate of 30%. The mean percentage questionnaire score ± SD was 17.5 ± 15.1. Scores were slightly higher for pharmacists with 2 or more pharmacokinetic classes in their formal education (p < 0.02). Conclusions: Understanding the principles of pharmacogenetics will allow pharmacists to appreciate that patients respond differently to certain medications as influenced by genetic variations encoding drug-metabolizing enzyme activity. As a consequence, some patients will have a normal therapeutic response, whereas others may experience drug toxicity or therapeutic inefficacy when given the same dose of a drug. This study determined, albeit with many limitations, that there is likely a need for improved availability of pharmacogenetic continuing education programs.

scholarly journals Study of Stereoselective Metabolism by Drug-metabolizing Enzyme Cytochrome P450

2007 ◽  
Vol 19 (Supplement) ◽  
pp. 210-210
Author(s):  
Aya Katsuura ◽  
Satoshi Matsuo ◽  
Yoshiko Nagata ◽  
Hideko Kanazawa
Keyword(s):  
Cytochrome P450 ◽  
Stereoselective Metabolism ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme
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