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Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells

التفاصيل البيبلوغرافية
العنوان: Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells
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
الوصف
تدمد:14756366
14756374
DOI:10.1080/14756366.2022.2163242