Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors,ACS Medicinal Chemistry Letters

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Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-09-24 , DOI: 10.1021/acsmedchemlett.0c00353
Christopher M Brackett ₁ , Ana García-Casas _{2,

3} , Sonia Castillo-Lluva _{2,

3} , Brian S J Blagg ₁

Affiliation

SUMOylation has emerged as an important post-translational modification that has been shown to modulate protein activity associated with various signaling pathways, and consequently, it has emerged as an important therapeutic target. While several natural products have been shown to inhibit enzymes involved in the SUMOylation process, there has been little progress toward the development of more selective and potent SUMOylation inhibitors. Ginkgolic acid was one of the first natural products discovered to inhibit the SUMO E1 enzyme. Despite its use to mechanistically investigate the SUMOylation process, ginkgolic acid also modulates other pathways as well. In this Letter, preliminary structure–activity relationships for ginkgolic acid as a SUMOylation inhibitor are presented.

中文翻译：

SUMO化抑制剂银杏酸衍生物的合成与评价

SUMOylation 已成为一种重要的翻译后修饰，已被证明可调节与各种信号通路相关的蛋白质活性，因此，它已成为重要的治疗靶点。虽然几种天然产物已被证明可以抑制参与 SUMOylation 过程的酶，但在开发更具选择性和效力的 SUMOylation 抑制剂方面进展甚微。银杏酸是最早发现的可抑制 SUMO E1 酶的天然产物之一。尽管它用于机械研究 SUMO 化过程，银杏酸也调节其他途径。在这封信中，介绍了银杏酸作为 SUMO 化抑制剂的初步构效关系。

更新日期：2020-11-12

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