دورية أكاديمية
Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells.
| العنوان: | Designing a Small Fluorescent Inhibitor to Investigate Soluble Epoxide Hydrolase Engagement in Living Cells. |
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| المؤلفون: | Brunst S; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Schönfeld J; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Breunig P; Buchmann Institute for Molecular Life Sciences and Institute for Cell Biology and Neuroscience, Goethe University Frankfurt, Max-von-Laue-Strasse 15, 60438 Frankfurt, Germany., Burgers LD; Institute of Pharmaceutical Biology, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., DeMeglio M; Buchmann Institute for Molecular Life Sciences and Institute for Cell Biology and Neuroscience, Goethe University Frankfurt, Max-von-Laue-Strasse 15, 60438 Frankfurt, Germany., Ehrler JHM; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Lillich FF; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Weizel L; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Hefendehl JK; Buchmann Institute for Molecular Life Sciences and Institute for Cell Biology and Neuroscience, Goethe University Frankfurt, Max-von-Laue-Strasse 15, 60438 Frankfurt, Germany., Fürst R; Institute of Pharmaceutical Biology, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Proschak E; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany., Hiesinger K; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt, Germany. |
| المصدر: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 Jun 14; Vol. 13 (7), pp. 1062-1067. Date of Electronic Publication: 2022 Jun 14 (Print Publication: 2022). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: Washington, D.C. : American Chemical Society |
| مستخلص: | Soluble epoxide hydrolase (sEH) is a promising target for a number of inflammation-related diseases. In addition, inhibition of sEH has been shown to reduce neuroinflammation, which plays a critical role in the development of central nervous system (CNS) diseases such as Alzheimer's disease. In this study, we present the rational design of a small fluorescent sEH inhibitor. Starting from the clinical candidate GSK2256294A, we replaced the triazine moiety with the 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole (NBD-Cl) fluorophore. The resulting fluorescent sEH inhibitor displayed excellent potency in an in vitro enzyme activity assay (IC Competing Interests: The authors declare no competing financial interest. (© 2022 The Authors. Published by American Chemical Society.) |
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| تواريخ الأحداث: | Date Created: 20220721 Latest Revision: 20230715 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC9290038 |
| DOI: | 10.1021/acsmedchemlett.2c00073 |
| PMID: | 35859883 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1948-5875 |
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| DOI: | 10.1021/acsmedchemlett.2c00073 |