教育背景:

2001－2006	美國波士頓大學	博士（有機合成化學）	導師：John Porco 教授
1997－2001	beat365	理學學士（化學）	導師：王劍波 教授

工作背景:

2017－現在	beat365 化學學院	新體制長聘正教授, 博士生導師
2014－現在	北大-清華生命科學聯合中心	高級研究員
2014－2017	beat365 化學學院	特聘研究員with tenure ，博士生導師
2013－2014	北京生命科學研究所	高級研究員
2008－2012	北京生命科學研究所	研究員, 化學中心主任
2008－2013	天津大學 藥學院	副教授, 教授
2006－2008	美國哥倫比亞大學	博士後（生物有機化學） 合作導師：Samuel Danishefsky 教授

學術獎勵:

• Bristol Myers Squibb Lectureship, Yale University, 2025
• Distinguished Visiting Professorship, Kyoto University, 2024
• Sackler Chair Visiting Scholar Award, Israel, 2023
• 科學探索獎，2022
• 屠呦呦獎，2022
• Boehringer-Ingelheim Senior Faculty Research Award, 2021
• Novartis Most Valuable Partner Award, 2021
• 教育部長江學者特聘教授，2021
• Bayer Investigator Award, 2020
• 樹蘭醫學青年獎，2019
• 北京市“卓越青年科學家”計劃，2018
• David Ginsburg Award, 2018
• 中國化學會-巴斯夫青年知識創新獎，2018
• Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017
• Swiss Chemical Society Distinguished Lectureship Award, 2017
• KAIST School of Molecular Science Lectureship Award, 2017
• 國家傑出青年科學基金, 2016
• Asian Core Program Lectureship Award, 2016
• Distinguished Lectureship Award by Chemical Society of Japan (CSJ), 2015
• 中國化學會-"維善天然産物合成獎"，2015
• 中組部萬人計劃-青年拔尖人才，2015
• Roche Young Investigator Award, 2014
• 北京市優秀青年人才，2014
• 科技部中青年科技創新領軍人才，2013
• 中國化學會"青年化學獎"，2013
• 國際化學生物學協會（ICBS）首屆"Young Chemical Biologist Award"，2013
• 中國藥學會"施維雅青年藥物化學獎"，2013
• Thieme Chemistry Journal Award, 2013
• Asian Core Program Lectureship Award, 2012
• 國家優秀青年科學基金, 2012
• 教育部新世紀優秀人才, 2010
• 藥明康德生命化學傑出科研獎, 2010
• IUPAC Young Chemist Award, 2009
• NESACS-JCF/GDCh Exchange Scholarship, 2005
• Sugata Ray Memorial Award for Excellence in Research at Boston University, 2005

研究領域：

有機合成、化學生物學、生物催化、合成生物學、創新藥物研發

研究方向：

小分子影響了許多重要的生物過程，因此它們可以被認為是生物中心法則的另一個重要的組成成分。具有生物活性的小分子可以是通過自然進化選擇的天然産物，也可以是通過有機合成制造的藥物分子和化學探針。我們課題組緻力于發展和應用新穎的活性小分子和化學技術去系統深入地研究重要生命過程，闡明與人類重大疾病密切相關的生物信号轉導通路中新的分子作用機制，去驗證全新的藥物靶點，從而幫助解決重大生物醫學難題。具體研究内容包括以下五個方面：

• 利用化學生物學手段研究與人類重大疾病（如：癌症，感染性疾病，神經退行性疾病等）相關的生物通路分子作用機制和調控方法；
• 開展複雜天然産物合成研究，并且運用活性天然産物發現新的生物靶點和闡明新的生物作用機制；
• 研究複雜天然産物生物合成，揭示新的酶學機制，并且綜合運用合成化學與合成生物學手段高效制備天然産物來源的藥物分子；
• 開發新一代高效的生物相容反應，并且利于化學交聯結合質譜技術系統研究複雜蛋白質結構和蛋白-蛋白相互作用；
• 尋找和發現新的藥物靶點，利用藥物化學手段開發創新型藥物。

代表性論文：

1. Pei Miao, Haijun Wang, Wei Wang, Zhengdong Wan, Han Ke, Hangyuan Chen, Jinjing Ni, Jingnan Liang, Yu-Feng Yao, Jizong Wang, Jian-Min Zhou*, and Xiaoguang Lei*“A widespread plant defense compound disarms bacterial type III injectisome assembly” Science 2025, 387, eads0377 (Highlighted by C&E News)
2. Jun Yang, Tianjun Zhao, Junping Fan, Huaibin Zou, Guangyi Lan, Fusheng Guo Yaocheng Shi, Han Ke, Huasheng Yu, Zongwei Yue, Xin Wang, Yingjie Bai, Shui Li, Yingjun Liu, Xiaoming Wang, Yu Chen*, Yulong Li*, Xiaoguang Lei* “Structure-guided discovery of bile acid derivatives for treating liver diseases without causing itch” Cell 2024, 187, 7164–7182 (Highlighted by C&E News)
3. Lei Li, Zhengping Ge, Shihao Liu, Kun Zheng, Yaqi Li, Kaiqi Chen, Yesheng Fu, Xiaoguang Lei, Zeling Cui, Yifan Wang, Jin Huang, Yanyan Liu, Mingwang Duan, Zimei Sun, Jun Chen, Liangwei Li, Pan Shen, Guibin Wang, Junmiao Chen, Ruochong Li, Chaoran Li, Zhixiang Yang, Yifan Ning, Arong Luo, Baoyu Chen, Inge Seim, Xin Liu,  Fei Wan, Yishan Yao, Fusheng Guo, Maojun Yang, Cui Hua Liu, Guangyi Fan*, Lizhi Wang*, Dong Yang*, Lingqiang Zhang* “Multi-omics landscape and molecular basis of radiation tolerance in a tardigrade” Science 2024, 386, eadl0799
4. Haoran Dong, Nianxin Guo, Dachao Hu, Benke Hong, Daohong Liao, Hong Jie Zhu, Zhang Yuan Yan, Hui Ming Ge, Xiaoguang Lei* “Chemoenzymatic Total Synthesis of Alchivemycin A” Nature Synthesis, 2024, 3, 1124-1133 (Highlighted by C&E News)
5. Lei Gao, Qi Ding, Xiaoguang Lei* “Hunting for the intermolecular Diels-Alderase” Acc. Chem. Res. 2024, 57, 2166–2183 (Cover article)
6. Bin Jiang, Lei Gao, Haijun Wang, Yaping Sun, Xiaolin Zhang, Han Ke, Shengchao Liu, Pengchen Ma, Qinggang Liao, Yue Wang, Huan Wang, Yugeng Liu, Ran Du, Torben Rogge, Wei Li, Yi Shang, K. N. Houk, Xingyao Xiong, Daoxin Xie, Sanwen Huang, Xiaoguang Lei*, Jianbin Yan* “Characterization and heterologous reconstitution of Taxus biosynthetic enzymes leading to baccatin III” Science 2024, 383, 622-629. (Highlighted by C&E News)
7. Kai Wang, Zhiwei Zhang, Jing Hang, Jia Liu, Fusheng Guo, Yong Ding, Meng Li, Qixing Nie, Jun Lin, Yingying Zhuo, Lulu Sun, Qihang Zhong, Chuan Ye, Chuyu Yun, Yi Zhang, Jue Wang, Rui Bao, Yanli Pang, Guang Wang*, Frank J. Gonzalez*, Xiaoguang Lei*, Jie Qiao*, Changtao Jiang* “Microbial-host-isozyme analyses reveal microbial DPP4 inhibition as a potential antidiabetic target”Science 2023, 381, eadd5787
8. Junping Fan, Linghan Hu, Zongwei Yue, Daohong Liao, Fusheng Guo, Han Ke, Daohua Jiang*, Yong Yang*, Xiaoguang Lei*  “Structural basis of TRPV3 inhibition by an antagonist” Nature Chemical Biology 2023, 19, 81-90
9. Jianyong Du, Lixia Zheng, Peng Gao, Hang Yang, Wan-Jie Yang, Fusheng Guo, Ruqi Liang, Mengying Feng, Zihao Wang, Zongwang Zhang, Linlu Bai, Ye Bu, Shijia Xing, Wen Zheng, Xuelian Wang, Li Quan, Xinli Hu, Haosen Wu, Zhixing Chen, Liangyi Chen, Ke Wei, Zhe Zhang, Xiaojun Zhu, Xiaolin Zhang, Qiang Tu, Shi-Min Zhao*, Xiaoguang Lei*, Jing-Wei Xiong* “A small-molecule cocktail promotes mammalian cardiomyocyte proliferation and heart regeneration” Cell Stem Cell 2022, 29, 545-558
10. Lei Gao, Yike Zou, Xiaojing Liu, Jun Yang, Xiaoxia Du, Jin Wang, Xinshui Yu, Junping Fan, Mingxuan Jiang, Yuli Li, K. N. Houk*, Xiaoguang Lei* “Enzymatic control of endo and exo stereoselective Diels-Alder reactions with broad substrate scope” Nature Catalysis 2021, 4, 1059-1069
11. Weilong Liu, Benke Hong, Jin Wang, Xiaoguang Lei* “New Strategies in the Efficient Total Syntheses of Polycyclic Natural Products” Acc. Chem. Res. 2020, 53, 2569–2586
12. Lei Gao, Cong Su, Xiaoxia Du, Ruishan Wang, Shuming Chen, Yu Zhou, Chengwei Liu, Xiaojing Liu, Runze Tian, Liyun Zhang, Kebo Xie, She Chen, Qianqian Guo, Lanping Guo, Yoshio Hano, Manabu Shimazaki, Atsushi Minami, Hideaki Oikawa, Niu Huang, K. N. Houk, Luqi Huang*, Jungui Dai*, Xiaoguang Lei* "FAD-dependent Enzyme-Catalysed Intermolecular [4+2] Cycloaddition in Natural Product Biosynthesis" Nature Chemistry, 2020, 12, 620-628. (Highlighted by Chemistry World)
13. Wang W, Yang J, Zhang J, Liu YX, Tian C, Qu B, Gao C, Xin P, Cheng S, Zhang W, Miao P, Li L, Zhang X, Chu J, Zuo J, Li J, Bai Y, Lei X,* Zhou JM* “An Arabidopsis Secondary Metabolite Directly Targets Expression of the Bacterial Type III Secretion System to Inhibit Bacterial Virulence” Cell Host & Microbe 2020, 27, 601–613
14. Bai, Y.; Lam, H.C.; Lei, X.*“Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, 53, 1034-1045
15. Wang J, Hong B, Hu D, Kadonaga Y, Tang R, Lei X.* “Protecting-Group-Free Syntheses of ent-Kaurane Diterpenoids: [3+2+1] Cycloaddition/Cycloalkenylation Approach.” J. Am. Chem. Soc. 2020, 142, 2238-2243
16. Sourav Banerjee, Tiantian Wei, Jue Wang, Jenna J. Lee, Haydee L. Gutierrez, Owen Chapman, Sandra E. Wiley, Joshua E. Mayfield, Vasudha Tandon, Edwin F. Juarez, Lukas Chavez, Ruqi Liang, Robert L. Sah, Caitlin Costello, Jill P. Mesirov, Laureano de la Vega, Kimberly L. Cooper, Jack E. Dixon*, Junyu Xiao*, and Xiaoguang Lei* “Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression” Proc. Natl Acad. Sci. USA 2019, 116, 24881-24891
17. Benke Hong, Weilong Liu, Jin Wang, Jinbao Wu, Yuichiro Kadonaga, Pei-Jun Cai, Hong-Xiang Lou, Zhixiang Yu, Houhua Li*, Xiaoguang Lei* “Photoinduced Skeletal Rearrangements Reveal Radical-Mediated Synthesis of Terpenoids” Chem 2019, 6,1671-1681 (Featured Article)
18. Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509
19. Liu, X.; Dong, T.; Zhou, Y.; Huang, N.; Lei, X.* “Exploring the Binding Proteins of Glycolipids with Bifunctional Chemical Probes” Angew. Chem. Int. Ed. 2016, 55, 14330-14334
20. Liao, D.; Yang, S.; Wang, J.; Zhang, J. Hong, B.; Wu, F.; Lei, X.* “Total Synthesis and Structural Reassignment of Aspergillomarasmine A” Angew. Chem. Int. Ed. 2016, 55, 4291-4295
21. Liu, W.; Li, H.; Cai, P.; Wang, Z.; Yu, Z-X.; Lei, X.* “Scalable Total Synthesis of Jungermannenones B and C” Angew. Chem. Int. Ed. 2016, 55, 3112-3116. (Highlighted by Synfacts 2016, 12, 0332)
22. Hong, B.; Li, C.; Wang, Z.; Chen, J.; Li, H.*; Lei, X.* “Enantioselective Total Synthesis of (-)-Incarviatone A” J. Am. Chem. Soc.2015, 137, 11946-11949. (News story describing this work was highlighted by Chem. & Eng. News 2015, 93, 35 and Synfacts 2015, 11, 1231)
23. Ren, R.; Zhou, X.; He, Y.; Ke, M.; Wu, J.; Liu, X.; Yan, C.; Wu, Y.; Gong, X.; Lei, X.; Yan, S. F.; Radhakrishnan, A.; Yan, N.* “Crystal structure of a mycobacterial Insig homolog provides insight into how these sensors monitor sterol levels” Science 2015, 349, 187-191
24. Hong, B.; Li, H.; Wu, J.; Zhang, J. Lei, X.* “Total Syntheses of (-)-Huperzine Q and (+)-Lycopladines B and C” Angew. Chem. Int. Ed. 2015, 54, 1011-1015. (Highlighted by Synfacts 2015, 11, 0112)
25. Han, J.; Li, X.; Guan, Y.; Zhao, W.; Wullf, W. D.*; Lei, X.* “Enantioselective Biomimetic Total Syntheses of Kuwanons I and J and Brosimones A and B” Angew. Chem. Int. Ed. 2014, 53, 9257-9261
26. Li, Q.; Dong, T.; Liu, X.; Lei, X.* “A Bioorthogonal Ligation Enabled by Click Cycloaddition of o-Quinolinone Quinone Methide and Vinyl Thioether” J. Am. Chem. Soc. 2013, 135, 4996-4999. (News story describing this work was highlighted in Chem. & Eng. News 2013, 14, 37)
27. Wang, G.*; Wang, X.; Yu, H.; Wei, S.; Williams, N.; Holmes, D. L.; Halfmann, R.; Naidoo, J.; Wang, L.; Li, L.; Chen, S.; Harran, P.; Lei, X.*; Wang, X.* “Small Molecule Activation of the TRAIL Receptor DR5 in Human Cancer Cells” Nature Chem. Biol. 2013, 9, 84-89. (News stories describing this work were highlighted in Chem. & Eng. News 2013, 2, 37; Nature Asia 2012, December 24)
28. Li, C.; Dian, L.; Zhang, W.; Lei, X.* “Biomimetic Syntheses of (-)-Gochnatiolides A-C and (-)-Ainsliadimer B” J. Am. Chem. Soc. 2012, 134, 12414-12417
29. Li, H.; Wang, X.; Lei, X.* “Total Syntheses of Lycopodium Alkaloids (+)-Fawcettimine, (+)-Fawcettidine and (-)-8-Deoxyserratinine” Angew. Chem. Int. Ed. 2012, 51, 491-495; Angew. Chem. 2012, 124, 506-510
30. Sun, L.; Wang, H.; Wang, Z.; He, S.; Chen, S.; Liao, D.; Wang, L.; Yan, J.; Liu, W.; Lei, X.*; Wang, X.* “Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of  RIP3 Kinase” Cell 2012, 148, 213-227. (News stories describing this work were highlighted in Chem. & Eng. News 2012, 5, 40; Nature China 2012, February 1; Asian Scientist 2012, January31; and Nature Reviews Molecular Cell Biology, 2012, Feb. 8)