摘要
SUMOylation 已成为一种重要的翻译后修饰,涉及小泛素样修饰符 (SUMO) 多肽与靶蛋白赖氨酸残基的共价连接。 SUMOylation 的酶促途径与泛素化非常相似,涉及激活酶、结合酶、连接酶和去结合酶。 SUMOylation 调节与各种途径相关的许多蛋白质的功能,事实上,在癌症和神经系统疾病中都观察到 SUMOylation 途径的失调。在许多癌症中,SUMO 酶被上调,SUMO 水平与预后和疾病进展直接相关。因此,SUMOylation 抑制剂的发现和开发受到了重视。在这篇综述中,描述了 SUMOylation 抑制剂的最新进展以及用于发现小分子 SUMOylation 抑制剂的方法,包括天然产物、肽模拟物以及通过虚拟屏幕识别的合成衍生物。
关键词: SUMO、癌症、泛素样、翻译后修饰、天然产物、小分子、酶抑制剂。
Current Medicinal Chemistry
Title:Current Status of SUMOylation Inhibitors
Volume: 28 Issue: 20
关键词: SUMO、癌症、泛素样、翻译后修饰、天然产物、小分子、酶抑制剂。
摘要: SUMOylation has emerged as an important post-translational modification that involves the covalent attachment of the Small Ubiquitin-like Modifier (SUMO) polypeptide to a lysine residue of a target protein. The enzymatic pathway of SUMOylation is very similar to ubiquitinylation and involves an activating enzyme, a conjugating enzyme, ligases, and deconjugating enzymes. SUMOylation modulates the function of a number of proteins associated with various pathways, and in fact, dysregulation of the SUMOylation pathway is observed in both cancer and neurological diseases. In many cancers, the SUMO enzymes are upregulated, and SUMO levels correlate directly with prognosis and disease progression. As a result, there has been an emphasis on the discovery and development of inhibitors of SUMOylation. In this review, the latest advances in SUMOylation inhibitors are described alongside the methods used to discover small molecule SUMOylation inhibitors, which include natural products, peptidomimetics, as well as synthetic derivatives identified via virtual screens.
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Cite this article as:
Current Status of SUMOylation Inhibitors, Current Medicinal Chemistry 2021; 28 (20) . https://dx.doi.org/10.2174/0929867327666200810135039
DOI https://dx.doi.org/10.2174/0929867327666200810135039 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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