ArticleAnalytical biochemistry2011
Development of fluorescent substrates for microsomal epoxide hydrolase and application to inhibition studies.
Article in Analytical biochemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 23 citations in OpenAlex.
- Synthetic Epoxyeicosatrienoic Acid Mimics Protect Mesangial Cells from Sorafenib-Induced Cell Death.Molecules (Basel, Switzerland) · 2025Article
- The Generation of a Nanobody-Based ELISA for Human Microsomal Epoxide Hydrolase.International journal of molecular sciences · 2023Article
- PROTAC-Mediated Selective Degradation of Cytosolic Soluble Epoxide Hydrolase Enhances ER Stress Reduction.ACS chemical biology · 2023Article
- Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives.Acta pharmaceutica Sinica. B · 2022Review
- Relative Importance of Soluble and Microsomal Epoxide Hydrolases for the Hydrolysis of Epoxy-Fatty Acids in Human Tissues.International journal of molecular sciences · 2021Article
- Nanobody-based binding assay for the discovery of potent inhibitors of CFTR inhibitory factor (Cif).Analytica chimica acta · 2019Article
- Substrate and inhibitor selectivity, and biological activity of an epoxide hydrolase from Trichoderma reesei.Molecular biology reports · 2019Article
- LC-MS/MS Analysis of the Epoxides and Diols Derived from the Endocannabinoid Arachidonoyl Ethanolamide.Methods in molecular biology (Clifton, N.J.) · 2018Article
- In Vitro Metabolism of Oprozomib, an Oral Proteasome Inhibitor: Role of Epoxide Hydrolases and Cytochrome P450s.Drug metabolism and disposition: the biological fate of chemicals · 2017Article
- Rational Design of Potent and Selective Inhibitors of an Epoxide Hydrolase Virulence Factor from Pseudomonas aeruginosa.Journal of medicinal chemistry · 2016Article
- Inhibiting an Epoxide Hydrolase Virulence Factor from Pseudomonas aeruginosa Protects CFTR.Angewandte Chemie (International ed. in English) · 2015Article
- Cloning and characterization of a microsomal epoxide hydrolase from Heliothis virescens.Insect biochemistry and molecular biology · 2013Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The microsomal epoxide hydrolase (mEH) plays a significant role in the metabolism of numerous xenobiotics. In addition, it has a potential role in sexual development and bile acid transport, and it is associated with a number of diseases such as emphysema, spontaneous abortion, eclampsia, and several forms of cancer. Toward developing chemical tools to study the biological role of mEH, we designed and synthesized a series of absorbent and fluorescent substrates. The highest activity for both rat and human mEH was obtained with the fluorescent substrate cyano(6-methoxy-naphthalen-2-yl)methyl glycidyl carbonate (11). An in vitro inhibition assay using this substrate ranked a series of known inhibitors similarly to the assay that used radioactive cis-stilbene oxide but with a greater discrimination between inhibitors. These results demonstrate that the new fluorescence-based assay is a useful tool for the discovery of structure-activity relationships among mEH inhibitors. Furthermore, this substrate could also be used for the screening chemical library with high accuracy and with a Z' value of approximately 0.7. This new assay permits a significant decrease in labor and cost and also offers the advantage of a continuous readout. However, it should not be used with crude enzyme preparations due to interfering reactions.
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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.