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在哺乳动物细胞中,海洋二甲类向STING棕化

Wan-Chi Hsiao^1,2, Guang-Hao Niu³, Chen-Fu Lo³

¹Institute of Molecular and Genomic Medicine, National Health Research Institutes, Miaoli, 35053, Taiwan.

Communications chemistry

|July 18, 2023

概括

像excavatolide B (excB) 这样的天然产品是药物发现的关键. 这项研究确定了STING作为excB的直接目标,揭示了它抑制炎症信号的机制.

科学领域:

海洋天然产品化学海洋天然产品化学
化学生物学是化学生物学.
药物发现药物发现

背景情况:

布里亚兰类型的二类物质,就像挖掘物质B (excB) 一样,是具有治疗潜力的复杂天然产品.
它们复杂的结构对合成和生物活动的表征提出了重大挑战.
软珊瑚是各种海洋天然产品的丰富来源.

研究的目的:

为结构-活性关系 (SAR) 研究合成和鉴定excavatolide B (excB) 的类似物.
在哺乳动物细胞中识别excB的直接分子标.
阐明 excB 在调节细胞信号通路中的作用机制.

主要方法:

培养的软珊瑚Briareum stechei被用作可扩展的ExCB来源.
使用后期多样化和结构活动分析来生成功能性exB探针.
化学蛋白质组策略被用来识别excB的蛋白质标.
进行了生物化学测试,以确认目标参与和下游信号的抑制.

主要成果:

干扰素基因刺激器 (STING) 被确定为excB的直接目标.
发现excB的环氧激素弹头对于与STING的共价接触至关重要.
通过向Cys91.1,excB被证明可以抑制STING的棕化和下游信号传输,通过向Cys91.
开发了功能性excB探头,用于进一步的生物研究.

结论:

这项研究揭示了干扰基因刺激剂 (STING) 作为excavatolide B (excB) 的直接分子标.
作用机制包括在Cys91处对STING的共价修饰,抑制其信号传递.
这项工作扩大了共价性STING抑制剂的库,并为开发新疗法提供了基础.

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