Research Experience
2014 – now Boya Distinguished Professor, College of Chemistry and Molecular Engineering, Peking University, China
2014 – now Senior Principal Investigator, Peking-Tsinghua Center for Life Sciences, Peking University, China
2008 – 2014 Principal Investigator and Director of Chemistry Center, National Institute of Biological Sciences (NIBS), Beijing, China
2006 – 2008 Post-doctoral Fellow, Bioorganic Chemistry, Columbia University and Memorial Sloan-Kettering Cancer Center, New York, NY, USA
Advisor: Professor Samuel J. Danishefsky
2001 – 2006 Ph.D. in Organic Synthesis and Chemical Biology, Boston University, Boston, USA
Advisor: Professor John A. Porco, Jr.
1997 – 2001 B.S. in Chemistry Peking University, Beijing, China
Advisor: Professor Jianbo Wang
Awards
Bristol Myers Squibb Lectureship, Yale University, 2025
Distinguished Visiting Professorship, Kyoto University, 2024
Sackler Chair Visiting Scholar Award, Israel, 2023
MDPI Tu Youyou Award, 2022
Xplorer Prize, 2022
Boehringer-Ingelheim Senior Faculty Research Award, 2021
Novartis Most Valuable Partner Award, 2021
Cheung Kong Distinguished Scholar, 2021
Bayer Investigator Award, 2020
Shu Lan Young Medical Investigator Award, 2019
David Ginsburg Memorial Lectureship Award, Israel, 2018
CCS-BASF Young Investigator Award, 2018
Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017
Swiss Chemical Society Distinguished Lectureship Award, Switzerland, 2017
KAIST School of Molecular Science Lectureship Award, South Korea, 2017
Asian Core Program Lectureship Award, 2016
Organic Chemistry Frontier Emerging Investigator Award, 2016
National Distinguished Young Investigator Award, 2016
Wei Shan Natural Product Synthesis Award by Chinese Chemical Society, 2015
Chemical Society of Japan Distinguished Lectureship Award, 2015
Outstanding Young Talent Award of Beijing, 2014
Roche Young Investigator Award, 2014
National Leading Young Scientific Investigator Award, 2013
Chinese Chemical Society Prize for Young Scientists, 2013
Young Chemical Biologist Award by the International Chemical Biology Society (ICBS), 2013
Servier Young Investigator Award by Chinese Pharmaceutical Association, 2013
Thieme Chemistry Journal Award, 2013
Asian Core Program Lectureship Award, 2012
Outstanding Young Investigator Award by National Natural Science Foundation of China, 2012
New Century Excellent Talents in University Award, 2010
WuXi PharmaTech 2010 Life Science and Chemistry Award, 2010
IUPAC Young Chemist Award, 2009
NESACS-JCF/GDCh Exchange Scholarship to Germany, 2005
Travel Award for the Gordon Research Conference on Combinatorial Chemistry, 2005
Sugata Ray Memorial Award for Excellence in Research and Teaching at Boston University, 2005
Research Interests
Chemical Biology, Natural Product Synthesis, Biosynthesis/Biocatalysis, Drug Discovery
Using small molecules probes to dissecting fundamental cellular processes, such as programmed cell death
Using a combined efforts of synthetic chemistry and synthetic biology to prepare complex natural products with significant biological functions
Developing new chemical biology tools to explore complex protein structures and protein-protein interactions
Developing the first-in-class drug candidates for the treatment of cancers, infectious diseases and auto-immune diseases
Selected Publications
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)
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)
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
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)
Lei Gao, Qi Ding, Xiaoguang Lei* “Hunting for the intermolecular Diels-Alderase” Acc. Chem. Res. 2024, 57, 2166–2183 (Cover article)
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)
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
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
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
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
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
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)
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
Bai, Y.; Lam, H.C.; Lei, X.*“Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, 53, 1034-1045
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
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
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)
Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509
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
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
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)
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)
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
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)
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
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)
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)
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
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
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)