ArticleAnalytical biochemistry2013
Development of an HTS assay for EPHX2 phosphatase activity and screening of nontargeted libraries.
Article in Analytical biochemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- Trial
- A Comprehensive Analysis of Epoxide Hydrolase 2 (EPHX2) in Pan-Cancer.Cancer reports (Hoboken, N.J.) · 2025Article
- EPHX2 overexpression deters the advancement of clear cell renal cell carcinoma via lipid metabolism reprogramming.Frontiers in oncology · 2025Article
- Intradomain Allosteric Regulation of Soluble Epoxide Hydrolase by Its Substrates.International journal of molecular sciences · 2024Article
- Article
- Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.Journal of medicinal chemistry · 2024Article
- Soluble epoxide hydrolase maintains steady-state lipid turnover linked with autocrine signaling in peritoneal macrophages.iScience · 2023Article
- PROTAC-Mediated Selective Degradation of Cytosolic Soluble Epoxide Hydrolase Enhances ER Stress Reduction.ACS chemical biology · 2023Article
- EPHX2 Inhibits Colon Cancer Progression by Promoting Fatty Acid Degradation.Frontiers in oncology · 2022Article
- Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.Journal of medicinal chemistry · 2019Article
- N-Substituted amino acid inhibitors of the phosphatase domain of the soluble epoxide hydrolase.Biochemical and biophysical research communications · 2019Article
- Soluble Epoxide Hydrolase and Brain Cholesterol Metabolism.Frontiers in molecular neuroscience · 2019Review
- Prospective for cytochrome P450 epoxygenase cardiovascular and renal therapeutics.Pharmacology & therapeutics · 2018Review
- Dysregulation of soluble epoxide hydrolase and lipidomic profiles in anorexia nervosa.Molecular psychiatry · 2016Article
- Heavy chain single-domain antibodies to detect native human soluble epoxide hydrolase.Analytical and bioanalytical chemistry · 2015Article
- Inhibiting an Epoxide Hydrolase Virulence Factor from Pseudomonas aeruginosa Protects CFTR.Angewandte Chemie (International ed. in English) · 2015Article
- The 2014 Bernard B. Brodie award lecture-epoxide hydrolases: drug metabolism to therapeutics for chronic pain.Drug metabolism and disposition: the biological fate of chemicals · 2015Review
- Effect of soluble epoxide hydrolase polymorphism on substrate and inhibitor selectivity and dimer formation.Journal of lipid research · 2014Article
- Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.Bioorganic & medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
Abstract
The EPXH2 gene encodes soluble epoxide hydrolase (sEH), which has two distinct enzyme activities: epoxide hydrolase (Cterm-EH) and phosphatase (Nterm-phos). The Cterm-EH is involved in the metabolism of arachidonic acid epoxides that play important roles in blood pressure, cell growth, inflammation, and pain. While recent findings suggested complementary biological roles for Nterm-phos, research is limited by the lack of potent bioavailable inhibitors of this phosphatase activity. Also, a potent bioavailable inhibitor of this activity could be important in the development of therapy for cardiovascular diseases. We report herein the development of an HTS enzyme-based assay for Nterm-phos (Z'>0.9) using AttoPhos as the substrate. This assay was used to screen a wide variety of chemical entities, including a library of known drugs that have reached through clinical evaluation (Pharmakon 1600), as well as a library of pesticides and environmental toxins. We discovered that ebselen inhibits sEH phosphatase activity. Ebselen binds to the N-terminal domain of sEH (K(I)=550 nM) and chemically reacts with the enzyme to quickly and irreversibly inhibit Nterm-phos, and subsequently Cterm-EH, and thus represents a new class of sEH inhibitor.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.