一套用于评估 CREB 抑制剂的生物测定法。
A suite of bioassays to evaluate CREB inhibitors.
机构信息
Program in Chemical Biology, Department of Chemical Physiology and Biochemistry, Knight Cancer Institute, Oregon Health and Science University, Portland, OR, United States.
出版信息
Methods Enzymol. 2020;633:169-184. doi: 10.1016/bs.mie.2019.11.002. Epub 2019 Nov 22.
Abstract
The cyclic-AMP response element binding protein (CREB) is an important nuclear transcription factor and has been shown to be overexpressed and/or over-activated in many different cancer types, suggesting that targeting CREB is a novel approach for developing cancer therapies. Our lab discovered the first cell-permeable small molecule inhibitor of CREB, from which we further developed a potent CREB inhibitor with in vivo anti-cancer activity. In this article, we detailed our biochemical and cell-based bioassays to assess different small molecule CREB inhibitors.
摘要
环腺苷酸反应元件结合蛋白（CREB）是一种重要的核转录因子，已在许多不同类型的癌症中显示出过表达和/或过度激活，表明靶向 CREB 是开发癌症疗法的一种新方法。我们的实验室发现了第一个细胞通透性的 CREB 小分子抑制剂，在此基础上，我们进一步开发了一种具有体内抗癌活性的强效 CREB 抑制剂。在本文中，我们详细介绍了我们用于评估不同小分子 CREB 抑制剂的生化和基于细胞的生物测定。
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2
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3
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4
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J Med Chem. 2015 Jun 25;58(12):5075-87. doi: 10.1021/acs.jmedchem.5b00468. Epub 2015 Jun 5.
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