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结构分析显示,水分子调解了GPR99的自我激活

Miaofang Xiao¹, Xiaoling Bao², Yusheng Guo¹

¹The Affiliated Traditional Chinese Medicine Hospital, GMU-GIBH Joint School of Life Sciences, The Guangdong-Hong Kong-Macao Joint Laboratory for Cell Fate Regulation and Diseases, Guangzhou Medical University, Guangzhou Municipal and Guangdong Provincial Key Laboratory of Protein Modification and Disease, State Key Laboratory of Respiratory Disease, Guangzhou, Guangdong, China.

Communications biology

|January 30, 2026

概括

这就是GPR99受体.

科学领域:

结构生物学结构生物学
生物化学生物化学
药理学药理学是指药理学的学科.

背景情况:

G蛋白结合受体99 (GPR99) 是炎症性疾病的潜在治疗点.
当与Gq蛋白结合时,GPR99表现出显著的基础活性,但其激活机制尚未完全理解.

研究的目的:

为了确定人体GPR99的高分辨率结构,在无体状态下与miniGq复合.
阐明GPR99自我激活的机制及其结构基础.

主要方法:

使用冷电子显微镜 (cryo-EM) 来确定GPR99-miniGq复合物的结构.
为了验证发现,进行了功能性实验,包括基于结构的突变发生,以验证结果.

主要成果:

发现GPR99的第二个细胞外循环 (ECL2) 占据了orthosteric结合口袋,导致受体自我激活.
结构性水分子形成一个连接ECL2和结合口袋的极性网络,影响受体活性.
突变性实验证实了ECL2在GPR99细胞内信号转导中的关键作用.

结论:

该研究揭示了GPR99自我激活的结构基础,通过其ECL2.2进行介导.
这些发现为理解GPR99功能和设计针对GPR99的药物提供了框架.

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