Exploring the Binding Proteins of Glycolipids with Bifunctional Chemical Probes |
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| Authors: | Xiaohui Liu Ting Dong Yu Zhou Prof. Dr. Niu Huang Prof. Dr. Xiaoguang Lei |
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| Affiliation: | 1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China;2. http://www.chem.pku.edu.cn/leigroup/;3. 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, China;4. National Institute of Biological Sciences (NIBS), Changping District, Beijing, China |
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| Abstract: | Glycolipids are important structural components of biological membranes and perform crucial functions in living systems, including signaling transduction and interaction with extracellular environment. However, the mechanistic exploration of glycolipids in vivo is challenging because they are not genetically encoded. Herein, we designed and synthesized a series of bifunctional monogalactosyldiacylglycerol (MGDG) probes as a model by introducing diazirine and terminal alkyne moieties on an aliphatic chain. In combination with proteome profiling and molecular modeling, we have demonstrated that MGDG alleviates inflammation by antagonizing TLR4. |
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| Keywords: | click chemistry glycolipids minimalist linker photoaffinity labeling target identification |
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