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Last update 08 May 2025

CYP2E1

Last update 08 May 2025

Basic Info

Synonyms

4-nitrophenol 2-hydroxylase, CYP2E, CYP2E1

+ [6]

Introduction

A cytochrome P450 monooxygenase involved in the metabolism of fatty acids (PubMed:10553002, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10553002, PubMed:18577768). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates fatty acids specifically at the omega-1 position displaying the highest catalytic activity for saturated fatty acids (PubMed:10553002, PubMed:18577768). May be involved in the oxidative metabolism of xenobiotics (Probable).

Drugs associated with CYP2E1

HUEXC-030

Target

Amidohydrolases x CYP2E1

Mechanism

Amidohydrolases inhibitors [+1]

Active Org.-

Originator Org.

Orient Pharma Co., Ltd.

Active Indication-

Inactive Indication

Tuberculosis

Drug Highest PhaseSuspended

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with CYP2E1

100 Translational Medicine associated with CYP2E1

0 Patents (Medical) associated with CYP2E1

6,049

Literatures (Medical) associated with CYP2E1

31 Dec 2025·Epigenetics

Acetaldehyde-driven mRNA methylation and expression changes in ethanol-metabolizing enzyme genes

Article

Author: Zhan, Qiansheng ; Zhang, Huiping ; Koo, Ji Sun

This study examines how the alcohol metabolite acetaldehyde modulates mRNA methylation and expression of ethanol-metabolizing genes, uncovering its epigenetic role in ethanol metabolism. Using neuron-like (SH-SY5Y) and non-neuronal (SW620) cellular models, we examined the effects of chronic intermittent acetaldehyde (CIA) exposure and subsequent withdrawal (CIA+WD) on global RNA m6A modifications and the methylation and expression of three brain ethanol-metabolizing genes: CAT (catalase), CYP2E1 (cytochrome P450 2E1), and ALDH2 (aldehyde dehydrogenase 2). A 3-week CIA exposure, with or without 24-hour withdrawal, did not significantly alter global m6A methylation levels in either cell line. However, acetaldehyde exposure/withdrawal induced hypermethylation at the mRNA stop codon regions of ALDH2 (CIA: p = 0.002; CIA+WD: p = 0.055) and CAT (CIA: p = 0.077; CIA+WD: p = 0.036) in SH-SY5Y cells, but not in SW620 cells. Furthermore, ALDH2 mRNA expression was significantly upregulated in both cell types following exposure (SH-SY5Y: p = 0.073 [CIA] and 0.00002 [CIA+WD]; SW620: p = 0.0009 [CIA] and 0.00008 [CIA+WD]). In contrast, CYP2E1 mRNA methylation and the expression of CYP2E1 and CAT remained unchanged. These findings highlight the cell-specific epigenetic effects of acetaldehyde, particularly its role in modulating mRNA methylation and expression of ALDH2, a key enzyme in alcohol metabolism.

01 Jul 2025·Biochimie

Human prostacyclin and thromboxane synthases: Molecular interactions, regulation, and pharmacology

Review

Author: Ershov, Pavel V ; Yablokov, Evgeniy O ; Mezentsev, Yuri V ; Ivanov, Alexis S

Prostanoids are lipid mediators of the human body that are involved in the inflammation and platelet aggregation. Prostacyclin is a vasodilator and inhibitor of platelet aggregation, and a product of the enzymatic reaction catalyzed by prostacyclin synthase (PTGIS). Thromboxane is a vasoconstrictor and synthesized by thromboxane synthase (TBXAS1). An imbalance of prostanoids can accompany cardio-/cerebrovascular diseases and cancers. PTGIS and TBXAS1 are clinically relevant membrane-bound enzymes of the multigene family of cytochromes P450 (CYPs), also known as CYP8A1 and CYP5A1, respectively. Particular studies of these functional antagonists will contribute to the elucidation of pathogenic mechanisms. The purpose of this work was to analyze the literature landscape over a period of 2020-2024 in the field of biological, pharmacogenomic, and pharmacological features of PTGIS and TBXAS1 as well as to explore the potential of their regulation at the post-transcriptional and post-translational levels using systems biological analysis. The review discusses recent findings on the novel aspects of both synthases established in gene knockout and overexpression experiments, current preclinical pharmacology, and potential ways of gene expression regulation. Identification of protein-protein interactions and post-translational modifications appear to be the main options for modulating PTGIS and TBXAS1 activity. The microsomal CYPs are known to form complexes with each other and direct interactions of CYP2E1 with both synthases can probably lead to modulation of their activity. Progress in the preclinical development of low molecular weight compounds as inhibitors of TBXAS1 is more prospective than PTGIS that is applied as gene therapy biologicals for in vivo production of prostacyclin due to its noticeable anticancer and vasodilator effects.

01 Jun 2025·Neoplasia

High dose acetaminophen re-polarizes CD11b+ cells in the tumor microenvironment towards an activated macrophage phenotype

Article

Author: May, Lauren ; Bryan, Allyn ; Lee, Won Sok ; Pingali, Pavani ; Shah, Syed A ; Khader, Adam ; Landry, Joseph ; Galabow, Andrea ; Martin, Rebecca K ; Lorenz, Madelyn ; Neuwelt, Alex ; Isbell, Madison ; Koblinski, Jennifer ; Patel, Bhaumik

OBJECTIVEHigh dose acetaminophen (AAP) has demonstrated promising results in early phase clinical trials for treatment of advanced malignancies. When administered concurrently with the CYP2E1 inhibitor fomepizole, AAP can be dose-escalated 100-fold relative to standard dosing without liver toxicity and without compromising anti-tumor activity.METHODS AND ANALYSISThe current study used a 23-plex flow cytometry panel to study AAP-induced changes in the tumor immune microenvironment of syngeneic mouse breast tumors. Effects of AAP on macrophage function and antigen presentation, alone and in combination with PD-1 antibodies, were evaluated.RESULTSFindings demonstrated that the vast majority of CD45+ cells in the triple negative breast cancer model are CD11b+ cells of the innate immune system. The CD11b+ cells in the tumor micro-environment of vehicle-treated mice were mostly comprised of GR1+ myeloid derived suppressor cells. On the other hand, the CD11b+ cells in the high dose AAP-treated mice were mostly of the activated macrophage phenotype (F4/80+CD80+MHCII+). In vitro studies were performed to better understand AAP effects on macrophage function. It was demonstrated that AAP enhances phagocytosis as well as antigen presentation by macrophages to antigen-reactive T-cells. These effects are amplified when PD-1 antibodies are combined with AAP in the in vitro antigen presentation assay. Furthermore, AAP has synergistic anti-tumor activity in vivo when combined with PD-1 antibody therapy, an effect that is macrophage dependent.CONCLUSIONThe present study demonstrates profound AAP-induced changes in the tumor immune microenvironment including the differentiation of CD11b+ cells towards an activated "M1" macrophage phenotype.

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CYP2E1

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