The human sirtuin silent information regulator 1 (SIRT1) is a NAD+-dependent deacetylase enzyme. It deacetylates many protein substrates, including histones and transcription factors, thereby controlling many physiological and pathological processes. Several synthetic inhibitors and activators of SIRT1 have been developed, and some therapeutic applications have been explored. The indole EX-527 and its derivatives are among the most potent and selective SIRT1 inhibitors. EX-527 has been often used as a pharmacological tool to explore the effect of SIRT1 inhibition in various cell types. Its therapeutic potential has, therefore, been evaluated in animal models for several pathologies, including cancer. It has also been tested in phase II clinical trial for the treatment of Huntington's disease (HD). In this review, we will provide an overview of the literature on EX-527, including its mechanism of inhibition and biological studies.

中文翻译：

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EX-527（SEN0014196或selisistat）抑制沉默信息调节因子1（SIRT1）的生化机制和生物学效应。

人沉默调节蛋白沉默信息调节剂1（SIRT1）是NAD +依赖性脱乙酰基酶。它使许多蛋白质底物（包括组蛋白和转录因子）脱乙酰，从而控制许多生理和病理过程。已经开发了几种SIRT1的合成抑制剂和活化剂，并且已经探索了一些治疗应用。吲哚EX-527及其衍生物是最有效和最具选择性的SIRT1抑制剂。EX-527通常被用作药理学工具，以研究SIRT1抑制在各种细胞类型中的作用。因此，已在动物模型中评估了其包括癌症在内的几种病理学的治疗潜力。它还已在II期临床试验中测试过，用于治疗亨廷顿舞蹈病（HD）。在这篇评论中