Probing the Anticancer Mechanism of (−)‐Ainsliatrimer A through Diverted Total Synthesis and Bioorthogonal Ligation |
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| Authors: | Dr Chao Li Ting Dong Qiang Li Prof?Dr Xiaoguang Lei |
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| Institution: | 1. Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Synthetic and Functional Biomolecules Center and Peking‐Tsinghua Center for Life Sciences, Peking University, Beijing 100871 (China) http://www.chem.pku.edu.cn/leigroup/;2. Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100730 (China);3. National Institute of Biological Sciences (NIBS), Changping District, Beijing 102206 (China) |
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| Abstract: | Herein, we report an efficient approach for exploring the novel anticancer mechanism of (?)‐ainsliatrimer A, a structurally complex and unique trimeric sesquiterpenoid, through a combined strategy of diverted total synthesis (DTS) and bioorthogonal ligation (TQ ligation), which allowed us to visualize the subcellular localization of this natural product in live cells. Further biochemical studies facilitated by pretarget imaging revealed that PPARγ, a nucleus receptor, was a functional cellular target of ainsliatrimer A. We also confirmed that the anticancer activity of ainsliatrimer A was caused by the activation of PPARγ. |
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| Keywords: | antitumor agents bioorganic chemistry bioorthogonal ligation diverted total synthesis target identification |
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