دورية أكاديمية
Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells
العنوان: | Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells |
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المؤلفون: | Aide Negri, Marina Marozzi, Daniela Trisciuoglio, Dante Rotili, Antonello Mai, Federica Rizzi |
المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023) |
بيانات النشر: | Taylor & Francis Group, 2023. |
سنة النشر: | 2023 |
المجموعة: | LCC:Therapeutics. Pharmacology |
مصطلحات موضوعية: | GSK126, JQ1, c-myc, metastatic prostate cancer, epigenetic drugs, Therapeutics. Pharmacology, RM1-950 |
الوصف: | AbstractAndrogen deprivation therapy (ADT) is a common treatment for recurrent prostate cancer (PC). However, after a certain period of responsiveness, ADT resistance occurs virtually in all patients and the disease progresses to lethal metastatic castration-resistant prostate cancer (mCRPC). Aberrant expression and function of the epigenetic modifiers EZH2 and BET over activates c-myc, an oncogenic transcription factor critically contributing to mCRPC. In the present work, we tested, for the first time, the combination of an EZH2 inhibitor with a BET inhibitor in metastatic PC cells. The combination outperformed single drugs in inhibiting cell viability, cell proliferation and clonogenic ability, and concomitantly reduced both c-myc and NF-kB expression. Although these promising results will warrant further in vivo validation, they represent the first step to establishing the rationale that the proposed combination might be suitable for mCRPC treatment, by exploiting molecular targets different from androgen receptor. |
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: | 10.1080/14756366.2022.2163242 |
URL الوصول: | https://doaj.org/article/23a51c8269fc43c7afe46977b921f61a |
رقم الأكسشن: | edsdoj.23a51c8269fc43c7afe46977b921f61a |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 14756366 14756374 |
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DOI: | 10.1080/14756366.2022.2163242 |