GPCR Activation and Endocytosis Induced by a 2D Material Agonist.
GPCR Activation and Endocytosis Induced by a 2D Material Agonist.
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DOI：
10.1021/acsami.7b02754
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发表时间：
2017-04
影响因子：
9.5
通讯作者：
Wei-Tao Dou;Yachao Kong;Xiao‐Peng He;Guorong Chen;Yi Zang;Jia Li;H. Tian
中科院分区：
文献类型：
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作者：
Wei-Tao Dou;Yachao Kong;Xiao‐Peng He;Guorong Chen;Yi Zang;Jia Li;H. Tian
激动剂诱导的G蛋白偶联受体（GPCR）的激活和内吞作用对于许多生理和病理过程至关重要。然而，可用于探测GPCR内吞作用的工具一直不足。本文通过κ-阿片受体（KOR）的内源性激动剂与二维二硫化钼的超分子自组装，制备了一种二维（2D）材料激动剂。2D物质激动剂已被证明适合于在稳定表达KOR的细胞中而不是在没有KOR表达的细胞中引发GPCR活化和内吞作用。使用超分辨率显微镜，我们还表明，2D材料激动剂共定位以及与GFP融合的KOR细胞内。此外，内吞的2D物质激动剂可以在过度表达KOR的细胞中选择性地产生活性氧，如通过光照射控制的。
Agonist-induced activation and endocytosis of G protein-coupled receptors (GPCRs) are crucial for a number of physiological and pathological processes. However, tools that are available for probing GPCR endocytosis have been insufficient. Here, we developed a two-dimensional (2D) material agonist by supramolecular self-assembly between an endogenous agonist of κ-opioid receptor (KOR) and 2D molybdenum disulfide. The 2D material agonist has proven to be amenable for eliciting GPCR activation and endocytosis in cells stably expressing KOR rather than in those without KOR expression. Using super-resolution microscopy, we also show that the 2D material agonist colocalizes well with GFP-fused KOR intracellularly. Further, the endocytosed 2D material agonist can selectively produce reactive oxygen species in cells that overly express KOR, as controlled by light irradiation.