دورية أكاديمية
Exploring the Ubiquitin-Proteasome System (UPS) through PROTAC Technology
| العنوان: | Exploring the Ubiquitin-Proteasome System (UPS) through PROTAC Technology |
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| المؤلفون: | Carlotta Cecchini, Sébastien Tardy, Valentina Ceserani, Jean-Philippe Theurillat, Leonardo Scapozza |
| المصدر: | CHIMIA, Vol 74, Iss 4, Pp 274-277 (2020) |
| بيانات النشر: | Swiss Chemical Society, 2020. |
| سنة النشر: | 2020 |
| المجموعة: | LCC:Chemistry |
| مصطلحات موضوعية: | protein degradation, proteolysis targeting chimeras, renal cell carcinoma, ubiquitylation, Chemistry, QD1-999 |
| الوصف: | In the context of dysregulated ubiquitylation, the accumulation of oncogenic substrates can lead to tumorigenesis. In particular, mutations in Von Hippel-Lindau (VHL) E3 ubiquitin ligase are related to overexpression of hypoxia-inducible factors (HIF-1α and HIF-2α) which is evolving into renal cell carcinoma (RCC). The classical approach of drug discovery focuses on the development of highly selective small molecules able to bind and to inhibit enzymatic active sites. This strategy faces limitations in the context of ' undruggable ' proteins, which are challenging to target. The discovery of Proteolysis Targeting Chimeras (PROTACs) as an alternative strategy to induce selective protein degradation is presented as a working hypothesis to understand further the UbiquitinProteasome System (UPS) and eventually counteract RCC cancer lacking VHL ubiquitin ligase. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | German English French |
| تدمد: | 0009-4293 2673-2424 |
| العلاقة: | https://www.ingentaconnect.com/contentone/scs/chimia/2020/00000074/00000004/art00012Test; https://doaj.org/toc/0009-4293Test; https://doaj.org/toc/2673-2424Test |
| DOI: | 10.2533/chimia.2020.274 |
| الوصول الحر: | https://doaj.org/article/0d58a029bbd34270b5cab9e09f786811Test |
| رقم الانضمام: | edsdoj.0d58a029bbd34270b5cab9e09f786811 |
| قاعدة البيانات: | Directory of Open Access Journals |
| تدمد: | 00094293 26732424 |
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| DOI: | 10.2533/chimia.2020.274 |