دورية أكاديمية
Replacing the phthalimide core in thalidomide with benzotriazole
| العنوان: | Replacing the phthalimide core in thalidomide with benzotriazole |
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| المؤلفون: | Mikhail Krasavin, Andrey Bubyrev, Alexander Kazantsev, Christopher Heim, Samuel Maiwald, Daniil Zhukovsky, Dmitry Dar’in, Marcus D. Hartmann, Alexander Bunev |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 527-530 (2022) |
| بيانات النشر: | Taylor & Francis Group, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | Cereblon, immunomodulatory drugs, phthalimide, benzotriazole, diazo compounds, carbene N-H insertion, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | The advent of proteolysis-targeting chimaeras (PROTACs) mandates that new ligands for the recruitment of E3 ligases are discovered. The traditional immunomodulatory drugs (IMiDs) such as thalidomide and its analogues (all based on the phthalimide glutarimide core) bind to Cereblon, the substrate receptor of the CRL4ACRBN E3 ligase. We designed a thalidomide analogue in which the phthalimide moiety was replaced with benzotriazole, using an innovative synthesis strategy. Compared to thalidomide, the resulting “benzotriazolo thalidomide” has a similar binding mode, but improved properties, as revealed in crystallographic analyses, affinity assays and cell culture. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 14756366 1475-6374 1475-6366 |
| Relation: | https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374 |
| DOI: | 10.1080/14756366.2021.2024525 |
| URL الوصول: | https://doaj.org/article/05018ca618a34ca08fb973d138964a14 |
| رقم الأكسشن: | edsdoj.05018ca618a34ca08fb973d138964a14 |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2021.2024525 |