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Synthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug

التفاصيل البيبلوغرافية
العنوان: Synthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug
المؤلفون: BoRa Lee, Dae Gyu Kim, Aram Lee, Young Mi Kim, Lianji Cui, Sunghoon Kim, Inhee Choi
المصدر: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1, Pp 51-66 (2023)
بيانات النشر: Taylor & Francis Group, 2023.
سنة النشر: 2023
المجموعة: LCC:Therapeutics. Pharmacology
مصطلحات موضوعية: PROTAC, AIMP2-DX2, lung cancer, Therapeutics. Pharmacology, RM1-950
الوصف: AbstractARS-interacting multifunctional proteins 2 (AIMP2) is known to be a powerful tumour suppressor. However, the target AIMP2-DX2, AIMP2-lacking exon 2, is often detected in many cancer patients and cells. The predominant approach for targeting AIMP-DX2 has been attempted via small molecule mediated inhibition, but due to the lack of satisfactory activity against AIMP2-DX2, new therapeutic strategies are needed to develop a novel drug for AIMP2-DX2. Here, we report the use of the PROTAC strategy that combines small-molecule AIMP2-DX2 inhibitors with selective E3-ligase ligands with optimised linkers. Consequently, candidate compound 45 was found to be a degrader of AIMP2-DX2. Together, these findings demonstrate that our PROTAC technology targeting AIMP2-DX2 would be a potential new strategy for future lung cancer treatment.
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: 10.1080/14756366.2022.2135510
URL الوصول: https://doaj.org/article/7b2ee4a801084b17b8b7db733202f13c
رقم الأكسشن: edsdoj.7b2ee4a801084b17b8b7db733202f13c
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14756366
14756374
DOI:10.1080/14756366.2022.2135510