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    Xiaoguang Lei,Ph.d 

      Department of Chemical Biology
      College of Chemistry and Molecular Engineering,  Peking University,
      Beijing 100871, P. R. China

     Address
     Room A509, 
     College of Chemistry and Molecular Engineering,
     Peking University, Beijing, 100871, China
     Contact
     Tel: +86-10-6276-0292
     Web:http://www.chem.pku.edu.cn/leigroup/
     Email：xglei@pku.edu.cn

 

Education

2001 – 2006    Ph.D. in Organic Synthesis and Chemical Biology       Boston University, Boston, USA

Advisor:  Professor John A. Porco, Jr.

Thesis: “Target and Diversity-Oriented Synthesis Using Epoxyquinoid Scaffolds”

1997 – 2001 B.S. in Chemistry      Peking University, Beijing, China

Advisor:  Professor Jianbo Wang

 

Professional Experience

2014 – Current    Professor, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, China

2008 – 2014    Principal Investigator and Director of Chemistry Center, National Institute of Biological Sciences (NIBS), Beijing, China

2010 – 2013     Professor, College of Pharmaceutical Science and Technology, Tianjin University

2008 – 2010     Associate Professor, College of Pharmaceutical Science and Technology, Tianjin University, 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

 

Honors and Awards

  • The Sackler Chair Award，2023
  • MDPI Tu Youyou Award, 2022
  • Xplorer Prize, 2022
  • Boehringer-Ingelheim Senior Faculty Research Award, 2021
  • Novartis Most Valuable Partner Award, 2021
  • Sackler Chair Visiting Scholar Award, Israel, 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,  

 

Affiliation

  • Member, International Chemical Biology Society (ICBS)
  • Member, Chinese-American Chemistry Professor Association (CAPA)
  • Member, American Chemical Society
  • Member, Chinese Chemical Society
  • Member, Chinese Pharmaceutical Association

 

Professional Service

Editor, Bioorganic and Medicinal Chemistry, 2017

Editorial Board Member, Bioorganic and Medicinal Chemistry (Letters), 2016-

Editorial Board Member, Advanced Science, 2015-

Editorial Board Member, Natural Product Research and Development, 2015-

Manuscript Referee

Nature (April 2020–Present)

Nature Chemical Biology (March 2013–Present)

Nature Cell Biology (April 2014–Present)

Nature Communication (October 2013–Present)

Cell Chemical Biology (September 2015–Present)

Angewandte Chemie, International Edition (July 2008–Present)

Chemical Communications (August 2008–Present)

Chemistry: A European Journal (December 2008–Present)

Chemistry: An Asian Journal (March 2009–Present)

European Journal of Organic Chemistry (November 2008–Present)

Organic and Biomolecular Chemistry (January 2010–Present)

Organic Letters (October 2008–Present)

Journal of the American Chemistry Society (August 2011–Present)

Journal of Organic Chemistry (January 2010–Present)

 

Research Interests

  • Chemical biology
  • Natural product synthesis
  • Synthetic biology
  • Drug discovery

 

Publications​

  1. Michelle McKee，Dongshan Wu, Jun Yang, Junping Fan, Jing-Ke Weng，Xiaoguang Lei*,The evolutionary origin of naturally occurring intermolecular Diels-Alderases from Morus alba，Qi Ding , Nianxin Guo , Lei Gao * , Nature Communications ，volume 15, Article number: 2492 (2024) 
  2. 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(6683),  622–629
  3. Chen, Peiqi，Li, Qiang*Lei, Xiaoguang*“Review of the impact of fragment-based drug design on PROTAC degrader discovery”Trends in Analytical Chemistry, 2024, 171, 117539
  4. Gao, Yihui，Ma, Mingzhe，Li, Wenyang*Lei, Xiaoguang*“Chemoproteomics, A Broad Avenue to Target Deconvolution”.Advanced Science, 2024, 11(8), 2305608
  5. Jun Yang, Kai Liang, Han Ke, Yuebin Zhang, Qian Meng, Lei Gao, Junping Fan, Guohui Li, Hu Zhou, Junyu Xiao*, and Xiaoguang Lei *"Enzymatic Degradation of Deoxynivalenol with the Engineered Detoxification Enzyme Fhb7”JACS Au Article ASAP
  6. Xiao, Fan,Sun, Mengze,Zhang, Liyun,Lei, Xiaoguang*”Investigation of Peptide Labeling with ortho-Phthalaldehyde and 2-Acylbenzaldehyde”Journal of Organic Chemistry, 2023
  7. Qixuan Wang, Fusheng Guo, Jin Wang and Xiaoguang Lei*“Divergent total syntheses of ITHQ-type bis-bcarboline alkaloids by regio-selective formal aza-[4+ 2] cycloaddition and late-stage C–H functionalization”Chemical Science 14,  37,  10353 - 1035913
  8. Kai Wang, Zhiwei Zhang, Jing Hang, Jia Liu, Fusheng Guo, Yong Ding, Meng Li, Qixing Nie,Jun Lin, Yingying Zhuo, Lulu Sun, Xi Luo, 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 as a potential antidiabetic target”Science, 2023, 381(6657), eadd5787
  9. Sanshan Wang, Kaiqi Chen, Fusheng Guo, Wenneng Zhu, Chendi Liu, Haoran Dong, Jin-Quan Yu,*and Xiaoguang Lei*“C−H Glycosylation of Native Carboxylic Acids: Discovery of Antidiabetic SGLT‑2 Inhibitors”ACS Central Science, 2023, 9(6),  1129–1139
  10. Jin Wang, Han Ke, Jun Yang, Nianxin Guo, Kangdelong Hu, Ruyao Tang,Qi Ding, Lei Gao*and Xiaoguang Lei*“Diversity-oriented synthesis of cyclohexenes by combining enzymatic intermolecular DielsAlder reactions and decarboxylative functionalizations”Chem Catalysis, 2023, 3(1), 100451
  11. Shijia Yuan, Lisha Xia, Chenxi Wang,Fan Wu, Bingjie Zhang, Chen Pan, Zhiran Fan, Xiaoguang Lei, Raymond C. Stevens, Andrej Sali, Liping Sun,* and Wenqing Shui* “Conformational Dynamics of the Activated GLP‑1 Receptor‑Gs Complex Revealed by Cross-Linking Mass Spectrometry and Integrative Structure Modeling”ACS Cent. Sci. 2023, 9, 5，992−1007 
  12. Haoran Dong, Dachao Hu, Benke Hong, Jin Wang, and Xiaoguang Lei*“Total Synthesis of Diverse Tetramic Acid Bearing cis-Decalin Natural Products”Angew. Chem. Int. Ed. 2023,62. e202301872
  13. Yuyue Qin , Linhu Zou , Xiaoguang Lei , Jiewei Su, Rixiu Yang , Wanjuan Xie ,Wanshan Li ,*, Guangying Chen *“OSMAC strategy integrated with molecular networking discovery peniciacetals A-I, nine new meroterpenoids from the mangrove-derived fungus Penicillium sp. HLLG-122” Bioorganic Chemistry；Volume 130, January 2023, 106271；
  14. 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 volume 19, pages81–90 (2023)
  15. Jin Wang, Han Ke, Jun Yang, Nianxin Guo, Kangdelong Hu, Ruyao Tang, Qi Ding, Lei Gao,* Xiaoguang Lei* “Diversity-oriented synthesis of cyclohexenes by combining enzymatic intermolecular Diels- Alder reactions and decarboxylative functionalizations” Chem Catal. 2023 3, 1–12
  16. 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 Chem. Biol. 2023, DOI: 10.1038/s41589-022-01166-5
  17. Yuyue Qin, Linhu Zou, Xiaoguang Lei, Jiewei Su, Rixiu Yang, Wanjuan Xie, Wanshan Li, Guangying Chen* “OSMAC strategy integrated with molecular networking discovery peniciacetals A-I, nine new meroterpenoids from the mangrove-derived fungus Penicillium sp. HLLG-122” Bioorg. Chem. 2023, 130, 106271
  18. Qihang Zhong, Honglei Chu, Guopeng Wang, Cheng Zhang, Rong Li, Fusheng Guo, Xinlu Meng, Xiaoguang Lei, Youli Zhou, Ruobing Ren, Lin Tao, Ningning Li, Ning Gao, Yuan Wei*, Jie Qiao*, Jing Hang* “Structural insights into the covalent regulation of PAPP-A activity by proMBP and STC2” Cell Discovery, 2022, 8, 137
  19. Fusheng Guo, Kaiqi Chen, Haoran Dong, Dachao Hu, Yihui Gao, Chendi Liu, Surat Laphookhieo, Xiaoguang Lei* “Biomimetic Total Synthesis and the Biological Evaluation of Natural Product (−)-Fargesone A as a Novel FXR Agonist” JACS Au 2022, DOI: 10.1021/jacsau.2c00600
  20. Fusheng Guo, Yihui Gao, Xiaobao Li*, Xiaoguang Lei* “Natural Product 2-Oxokolavenol Is a Novel FXR Agonist” Molecules 2022, 27, 8968
  21. Yongqing Yang*, Xiaohui Liu, Xin Wang, Wanjia Lv, Xiao Liu, Liang Ma, Haiqi Fu, Shu Song, Xiaoguang Lei* “Screening of protonstatin-1 (PS-1) analogs for improved inhibitors of plant plasma membrane H+-ATPase activity” Front. Plant Sci. 2022, 13, 973471
  22. Yingjie Bai, Tianhu Zhao, Mengyu Gao, Yuanqiang Zou, Xiaoguang Lei* “A Novel Gene Alignment in Dorea sp. AM58-8 Produces 7-Dehydroxy-3β Bile Acids from Primary Bile Acids” Biochemistry 2022, 61, 2870-2878
  23. Mengyue Deng, Yue Li, Yulu Li, Xiaolan Mao, Han Ke , Weiling Liang , Xiaoguang Lei, Yu-Lung Lau, Huawei Mao* “A Novel STAT3 Gain-of-Function Mutation in Fatal Infancy-Onset Interstitial Lung Disease” Front. Immunol. 2022,13, 866638
  24. Biwei Liu, Shentian Zhuang, Runze Tian, Yuan Liu, Yanqi Wang, Xiaoguang Lei*, Chu Wang* “Chemoproteomic Profiling Reveals the Mechanism of Bile Acid Tolerance in Bacteria” ACS Chem. Biol. 2022, 17, 2461-2470
  25. Dongshan Wu, Xiaoguang Lei* “Enzymatic cascade reactions for the efficient synthesis of natural products” Tetrahedron 2022, 127, 133099
  26. Mengze Sun, Fang Yuan, Yuliang Tang, Peng Zou*, Xiaoguang Lei* “Subcellular Interactomes Revealed by Merging APEX with Cross-Linking Mass Spectrometry” Anal. Chem. 2022, 94, 14878-14888.
  27. Ruiyu Xiang, Linghan Hu, Siyuan Li, Ziyu Wei, Zhongya Song, Zhiming Chen, Yihe Liu, Juan Liu, Xiaoguang Lei, Yong Yang* “Tiamulin inhibits TNF-α and alleviates psoriasis-like dermatitis” J. Dermatol. Sci. 2022, 107, 32-40
  28. Yange Niu, Wenhao Cui, Rui Liu, Sanshan Wang, Han Ke, Xiaoguang Lei, Lei Chen* “Structural mechanism of SGLT1 inhibitors” Nature  Commun. 2022, 13, 6440
  29. Wenyang Li, Jue Wang, Ruqi Liang, Xiaoguang Lei* “Perturbation of biological processes with small molecule kinase inhibitors” Current Opinion in Chemical Biology 2022, 70, 102185
  30. Lei Gao, Jun Yang, Xiaoguang Lei* “Enzymatic intermolecular Diels-Alder reactions in synthesis: From nature to design” Tetrahedron Chem 2022, 2, 100013
  31. 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
  32. Junxia Zhang, Ruqi Liang, Kai Wang, Wenjia Zhang, Mao Zhang, Li Jin, Peng Xie, Wen Zheng, Haibao Shang, Qingmei Hu, Jiayi Li, Gengjia Chen, Fujian Wu, Feng Lan, Lipeng Wang, Shi-Qiang Wang, Yongfeng Li, Yong Zhang, Jinghao Liu, Fengxiang Lv, Xinli Hu, Rui-Ping Xiao, Xiaoguang Lei*, Yan Zhang* “Hesperadin Is a Novel CaMKII-δ Inhibitor and Exerts Dual Functions to Both Protect Cardiac Ischemia/reperfusion Injury and Inhibit Tumor Growth” Circulation 2022, 145, 1154-1168
  33. Jun Zhang, Daohong Liao, Rongchang Chen, Fangfang Zhu, Yaqing Ma, Lei Gao, Ge Qu, Chengsen Cui, Zhoutong Sun*, Xiaoguang Lei*, Shu-Shan Gao* “Tuning an Imine Reductase for the Asymmetric Synthesis of Azacycloalkylamines by Concise Structure-Guided Engineering” Angew. Chem. Int. Ed. 2022, 61, e202201908.
  34. Zongwei Yue, Fan Wu, Fusheng Guo, Jiyeong Park, Jin Wang, Liyun Zhang, Daohong Liao, Wenyang Li, Orlando D Schärer, Xiaoguang Lei* “Polycarcin V induces DNA damage response and enables the profiling of DNA-binding proteins” National Science Review 2022, DOI: 10.1093/nsr/nwac046
  35. Yongqing Yang*, Xiaohui Liu, Wei Guo, Wei Liu, Wei Shao, Jun Zhao, Junhong Li, Qing Dong, Liang Ma, Qun He, Yingzhang Li, Jianyong Han, Xiaoguang Lei* “Testing the polar auxin transport model with a selective plasma membrane H + -ATPase inhibitor” J. Integr. Plant Biol. 2022, 64, 1229-1245
  36. Tiantian Wei, Jue Wang, Ruqi Liang, Wendong Chen, An He, Yifei Du, Wenjing Zhou, Zhiying Zhang, Mingzhe Ma, Jin Lu, Xing Guo, Xiaowei Chen, Youjun Wang, Ruijun Tian*, Junyu Xiao*, Xiaoguang Lei* “Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry” eLife 2022, 11: e77696
  37. Xueping Wang, Victor Tomilin, Merve Ertem, Abigail McKernan, Xiaoguang Lei, Oleh Pochynyuk, Ossama B Kashlan* “Bile acids regulate the epithelial Na+ channel in native tissues through direct binding at multiple sites” J. Physiol. 2022, 600, 4695-4711.
  38. Jian-Hua Wang, Yu-Liang Tan, Rohit Jain, Fan Xiao, Zhou Gong, Yu Zhou, Dan Tan, Qiang Li, Xu Dong, C. Robert Matthews, Shu-Qun Liu, Niu Huang, Keqiong Ye, Chun Tang*, Meng-Qiu Dong*, Xiaoguang Lei* “Characterization of protein unfolding by fast cross-linking mass spectrometry using di-ortho-phthalaldehyde cross-linkers” Nature Communications 2022, 13, 1468
  39. Bai J, Guo F, Li M, Li Y*, Lei X* “Click-based amplification: designed to facilitate various target labelling modes with ultralow background amplification” RSC Chem. Biol. 2021, 2, 906-916.
  40. Yang Y, Han X, Ma L, Wu Y, Liu X, Fu H, Liu G, Lei X*, Guo Y* “Dynamic changes of phosphatidylinositol and phosphatidylinositol 4-phosphate levels modulate H+-ATPase and Na+/H+ antiporter activities to maintain ion homeostasis in Arabidopsis under salt stress” Mol. Plant. 2021, 14, 2000-2014
  41. Ma G, Wang S, Wu K, Zhang W, Ahmad A, Hao Q*, Lei X*, Zhang H* “Structure-guided optimization of D-captopril for discovery of potent NDM-1 inhibitors” Bioorg. Med. Chem. 2021 29, 115902
  42. Bai Y, Zhang L, Lei X* “Human Endogenous Natural Products” Prog. Chem. Org. Nat. Prod. 2021, 114, 313-337.
  43. Sun DE, Fan X, Shi Y, Zhang H, Huang Z, Cheng B, Tang Q, Li W, Zhu Y, Bai J, Liu W, Li Y, Wang X, Lei X, Chen X.* “Click-ExM enables expansion microscopy for all biomolecules” Nature Methods 2021, 18, 107-113.
  44. 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
  45. Lei Gao*, Xiaoguang Lei* “Biosynthetic Intermediate Probes for Visualizing and Identifying the Biosynthetic Enzymes of Plant Metabolites” ChemBioChem 2021, 22, 982-984
  46. 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
  47. Tianhu Zhao, Jian Zhang, Xiaowan Han, Jun Yang, Xin Wang, Maarten Vercruysse, Hai-Yu Hu*, Xiaoguang Lei* “A Pseudopaline Fluorescent Probe for the Selective Detection of Pseudomonas aeruginosa” CCS Chemistry 2020, 2, 2405-2417
  48. Xiaojing Liu, Jun Yang, Lei Gao, Liyun Zhang, Xiaoguang Lei* “Chemoenzymatic Total Syntheses of Artonin I with an Intermolecular Diels–Alderase” Biotechnol. J. 2020, 15, 2000119
  49. Weilong Liu, Zongwei Yue, Zhen Wang, Houhua Li, Xiaoguang Lei* “Syntheses of Skeletally Diverse Tetracyclic Isodon Diterpenoid Scaffolds Guided by Dienyne Radical Cyclization Logic” Org. Lett. 2020, 22, 7991-7996
  50. Puzhong Lu, Rui Liu, Di Lu, Yue Xu, Xueyi Yang, Zheng Jiang, Chun Yang, Li Yu*, Xiaoguang Lei*, Yang Chen* “Chemical screening identifies ROCK1 as a regulator of migrasome formation” Cell Discovery 2020, 6, 51
  51. 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
  52. Qianqian Guo, Dongshan Wu, Lei Gao, Yingjie Bai, Yuan Liu, Nianxin Guo, Xiaoming Wang, Xiaoguang Lei* “Identification of the AMA synthase from the aspergillomarasmine A biosynthesis and evaluation of its biocatalytic potential” ACS Catalysis, 2020, 10, 6291-6298
  53. Wu, F.; Zhang, J.; Song, F.; Wang, S.; Guo, H.; Wei, .; Dai, H.; Chen, X.; Xia, X.; Liu, X.; Zhang, L.; Yu, J.-Q.; Lei, X.* “Chrysomycin A Derivatives for the Treatment of Multidrug Resistant Tuberculosis” ACS Cent. Sci. 2020, 6, 928-938
  54. 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
  55. Hong, B.; Luo, T.; Lei, X.* “Late-Stage Diversification of Natural Products” ACS Cent. Sci. 2020, 6, 622-635
  56. Bai, Y.; Lam, H.C.; Lei, X.* “Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, 53, 1034-1045
  57. Liu Q, Yu J, Wang L, Tang Y, Zhou Q, Ji S, Wang Y, Santos L, Haeusler RA, Que J, Rajbhandari P, Lei X, Valenti L, Pajvani UB,* Qin J,* Qiang L.* “Inhibition of PU.1 ameliorates metabolic dysfunction and non-alcoholic steatohepatitis” J. Hepatol. 2020, 73, 361-370
  58. Zhang X, Zhang SQ, Li Q, Xiao F, Yue Z, Hong X,* Lei X.* “Computation-Guided Development of the "Click" ortho-Quinone Methide Cycloaddition With Improved Kinetics” Org Lett. 2020, 22, 2920-2924
  59. 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.
  60. Meesakul P, Jaidee W, Richardson C, Andersen RJ, Patrick BO, Willis AC, Muanprasat C, Wang J, Lei X, Hadsadee S, Jungsuttiwong S, Pyne SG, Laphookhieo S.* “Styryllactones from Goniothalamus tamirensis” Phytochemistry 2020, 71, 112248
  61. Zongwei Yue, Hiu C. Lam, Kaiqi Chen, Ittipon Siridechakorn, Yaxi Liu, Khanitha Pudhom, Xiaoguang Lei* “Biomimetic synthesis of rhytidenone A and elucidation of mode of action of the cytotoxic rhytidenone F” Angew. Chem. Int. Ed.  2020, 59, 4115-4120
  62. Lisha Xia, Ziliang Ma, Jiahui Tong, Yuliang Tang, Shanshan Li, Shanshan Qin, Ronghui Lou, Suwen Zhao, Xiaoguang Lei*, Wenqing Shui* “Evaluation of chemical cross-linkers for in-depth structural analysis of G protein-coupled receptors through cross-linking mass spectrometry.” Analytica Chimica Acta 2019, 1102, 53-62
  63. 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
  64. Jeffrey S. McFarlane, Jian Zhang, Sanshan Wang, Xiaoguang Lei, Graham R. Moran, and Audrey L. Lamb* “Staphylopine and pseudopaline dehydrogenase from bacterial pathogens catalyze reversible reactions and produce stereospecific metallophores” J. Biol. Chem. 2019, 294, 17988-18001
  65. Huasheng Yu, Tianjun Zhao, Simin Liu, Qinxue Wu, Omar Johnson, Zhaofa Wu, Zihao Zhuang, Yaocheng Shi, Luxin Peng, Renxi He, Yong Yang, Jianjun Sun, Xiaoqun Wang, Haifeng Xu, Zheng Zeng, Peng Zou, Xiaoguang Lei, Wenqin Luo*, Yulong Li* “MRGPRX4 is a bile acid receptor for human cholestatic itch” eLife 2019, 8, e48431
  66. Alexander X. Jones, Yong Cao, Yu-Liang Tang, Jian-Hua Wang, Yue-He Ding, Hui Tan, Zhen-Lin Chen, Run-Qian Fang, Jili Yin, Rong-Chang Chen, Xing Zhu, Yang She, Niu Huang, Feng Shao , Keqiong Ye , Rui-Xiang Sun, Si-Min He , Xiaoguang Lei* & Meng-Qiu Dong* “Improving mass spectrometry analysis of protein structures with arginine-selective chemical cross-linker” Nature Comm. 2019, 10, 3911
  67. Jian Zhang, Tianhu Zhao, Rongwen Yang, Ittipon Siridechakorn, Sanshan Wang, Qianqian Guo, Yingjie Bai, Hong C. Shen, Xiaoguang Lei* “De novo synthesis, structural assignment and biological evaluation of pseudopaline, a metallophore produced by Pseudomonas aeruginosa” Chem. Sci. 2019, 10, 6635-6641
  68. Yaocheng Shi, Zhi Xu, Renxiang Tan, Xiaoguang Lei* “Divergent Total Synthesis of Chaetoglines C to F” J. Org. Chem. 2019, 84, 8766-8770
  69. 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)
  70. Jinbao Wu, Yuichiro Kadonaga, Benke Hong, Jin Wang, Xiaoguang Lei* “Enantioselective Total Synthesis of (+)-Jungermatrobrunin A” Angew. Chem. Int. Ed. 2019, 58, 10879-10883
  71. Tianhu Zhao, Jian Zhang, Maomao Tang, Luyan Z. Ma*, Xiaoguang Lei* “Development of an Effective Fluorescence Probe for Discovery of Aminopeptidase Inhibitors to Suppress Biofilm Formation” J. Antibiot. 2019，72，461-468
  72. Chen, K.; Lei, X.* Recent applications of C-H functionalization in complex molecule synthesis. Curr. Opin. Green Sustain. Chem. 2018, 11, 9-14
  73. Wu F, Zhang J, Shang E, Zhang J, Li X, Zhu B, Lei X.* “Synthesis and Evaluation of a New Type of Small Molecule Epigenetic Modulator Containing Imidazo[1,2-b][1,2,4]triazole Motif”  Front Chem. 2018, 6, 642
  74. Wang X, Du C, Hong B, Lei X.* “Total synthesis of (±)-antroquinonol”. Org. Biomol. Chem. 2018, 17, 1754-1757.
  75. Xiao F, Zhang X, Lei X.* “Recent Developments and Applications of Photoconjugation Chemistry”. Chimia 2018, 72, 782-790
  76. Zhu H, Zhang L, Wu Y, Dong B, Guo W, Wang M, Yang L, Fan X, Tang Y, Liu N, Lei X, Wu H.* “T-ALL leukemia stem cell 'stemness' is epigenetically controlled by the master regulator SPI1”. elife 2018, e38314
  77. Ye, Z.; Zhang, X.; Zhu, Y.; Song, T.; Chen, X.; Lei, X.*; Wang, X.* “Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function” Mol. Pharm. 2018, 15, 2413-2422
  78. Dong Q, Li X, Wang CZ, Xu S, Yuan G, Shao W, Liu B, Zheng Y, Wang H, Lei X, Zhang Z, Zhu B.* “Roles of the CSE1L-mediated nuclear import pathway in epigenetic silencing” Proc Natl Acad Sci U S A. 2018, 115, E4013-E4022
  79. Ozaki T, Shinde SS, Gao L, Okuizumi R, Liu C, Ogasawara Y, Lei X, Dairi T, Minami A, Oikawa H.* “Enzymatic formation of a skipped methyl-substituted octaprenyl side chain of longestin (KS-505a): Involvement of homo-IPP as a common extender unit” Angew. Chem. Int. Ed. 2018, 57, 6629-6632
  80. Li X, Shang E, Dong Q, Li Y, Zhang J, Xu S, Zhao Z, Shao W, Lv C, Zheng Y, Wang H, Lei X, Zhu B,* Zhang Z.* “Small molecules capable of activating DNA methylation-repressed genes targeted by the p38 mitogen-activated protein kinase pathway” J. Biol. Chem. 2018, 293, 7423-7436
  81. Gubu, A.; Li, L.; Ning, Y.; Zhang, X.; Lee, S.; Feng, M.; Li, Q.; Lei, X.; Jo, K.; Tang, X.* “Bioorthogonal Metabolic DNA Labelling using Vinyl Thioether-Modified Thymidine and o-Quinolinone Quinone Methide” Chem. Eur. J. 2018, 24, 5895-5900
  82. Yue, Z.; Xiao, X.; Wu, J.; Zhou, X.; Liu, W.; Liu, Y.; Li, H.; Chen, G.; Wu, Y.*; Lei, X.* “ent-Jungermannenone C Triggers Reactive Oxygen Species-Dependent Cell Differentiation in Leukemia Cells” J. Nat. Prod. 2018, 81, 298-306
  83. Zhang, X.; Wang, J.; Tan, D.; Li, Q.; Li, M.; Gong, Z.; Tang, C.; Liu, Z.; Dong, W.*; Lei, X.* “Carboxylate-Selective Chemical Cross-Linkers for Mass Spectrometric Analysis of Protein Structures” Anal. Chem. 2018, 90, 1195-1201
  84. Li, H.; Lei, X.* “Fawcettimine-Type Lycopodium Alkaloids as a Driving Force for Discoveries in Organic Synthesis” Chem. Rec. 2018, 18, 543-554
  85. Narita, K.; Sato, H.; Minami, A.; Kudo, K.; Gao, L.; Liu, C.; Ozaki, T.; Kodama, M.; Lei, X.; Taniguchi, T.; Monde, K.; Yamazaki, M.; Uchiyama, M.; Oikawa, H.* “Focused Genome Mining of Structurally Related Sesterterpenes: Enzymatic Formation of Enantiomeric and Diastereomeric Products” Org. Lett. 2017, 19, 6696-6699.
  86. Zhang, J.; Wang, S.; Bai, Y.; Guo, Q.; Zhou, J.; Lei, X.* “Total Syntheses of Natural Metallophores Staphylopine and Aspergillomarasmine A” J. Org. Chem. 2017, 82, 13643-13648.
  87. Zhang, J.; Wang, S.; Wei, Q.; Guo, Q.; Bai, Y.; Yang, S.; Song, F.; Zhang, L.; Lei, X.* “Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance.” Bioorg. Med. Chem. 2017, 25, 5133-5141.
  88. Han, X.; Yang, Y.; Wu, Y.; Liu, X.; Lei, X.*; Guo, Y.* “A bioassay-guided fractionation system to identify endogenous small molecules that activate plasma membrane H+-ATPase activity in Arabidopsis.” J. Exp. Bot. 2017, 68, 2951-2962.
  89. Hong, B.; Hu, D.; Wu, J.; Zhang, J.; Li, H.; Pan, Y.; Lei, X.* “Divergent Total Syntheses of (-)-Huperzine Q, (+)-Lycopladine B, (+)-Lycopladine C and (-)-epi-Lycopladine D” Chem. Asian J. 2017, 12, 1557-1567. (VIP paper)
  90. Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509.
  91. Jones, A.; Zhang, X.; Lei, X.* “Covalent Probe Finds Carboxylic Acid” Cell Chem. Biol. 2017, 24, 537-538.
  92. Ren, Y.; Su, Y.; Su, L.; He, S.; Meng, L.; Liao, D.; Liu, X.; Ma, Y.; Liu, C.; Li, S.; Ruan, H.; Lei, X.; Wang, X.*; Zhang, Z.* “Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome” J. Med. Chem. 2017, 60, 972-986.
  93. Siridechakorn, I.; Yue, Z.; Mittraphab, Y.; Lei, X.; Pudhom, K.* “Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B” Bioorg. Med. Chem. 2017, 25, 2878-2882.
  94. 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.
  95. Tan, D.; Li, Q.; Zhang, M.; Liu, C.; Ma, C.; Zhang, P.; Ding, Y.; Fan, S.; Tao, L.; Yang, B.; Li, X.; Ma, S.; Liu, J.; Feng, B.; Liu, X.; Wang, H.; He, S.; Gao, N.; Ye, K.; Dong, M.*; Lei, X.* “Trifunctional Cross-Linker for Mapping  Protein-Protein Interaction Networks and Comparing  Protein Conformational States” eLife 2016; 5:e12509. (News story describing this work was highlighted by Nature Methods 2016, 13, 392-392).
  96. Li, C.; Jones, A.; Lei, X.* “Synthesis and Mode of Action of Oligomeric Sesquiterpene Lactones” Nat. Prod. Rep. 2016, 33, 602-611. (Cover story)
  97. Shang, E.; Zhang, J.;  Bai, J.; Wang, Z.; Li, X.; Zhu, B.; Lei, X.* “Syntheses of [1,2,4]triazolo[1,5-a]benzazoles Enabled by the Transition-Metal-Free Oxidative N-N Bond Formation”  Chem. Commun. 2016, 52, 7028-7031.
  98. 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.
  99. 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).
  100. Li, D.; Li, C.; Li, L.; Chen. S.; Wang, L.; Li, Q.; Wang, X.; Lei, X.*; Shen, Z.* “Natural Product Kongensin A is a Non-Canonical HSP90 Inhibitor that Blocks RIP3-dependent Necroptosis” Cell Chem. Biol. 2016, 23, 257-266. (Featured article, and highlighted by Jacobsen et al. Cell Chem. Biol. 2016, 23, 205-207).
  101. Gao, L.; Han, J.; Lei, X.* “Enantioselective Total Syntheses of Kuwanon X, Kuwanon Y and Kuwanol A” Org. Lett. 2016, 18, 360-363.
  102. Yang, S.; Liao, D.; Tian, X.; Lei, X.* “Access to the 2H-tetrahydro-4, 6-dioxo-1, 2-oxazine Ring System from Nitrone via a Tandem Nucleophilic Addition and Transesterification Re-action” Org. Lett. 2016, 18, 376-379.
  103. Dong, T.; Liu, W.; Shen, Z.; Li, L.; Chen, S.; Lei, X.* “Pterisolic Acid B is a Nrf2 Activator by Targeting C171 within Keap1-BTB Domain” Sci. Rep. 2016, 6, 19231.
  104. Ma, K.; Liao, D.; Yang, S.; Li, X.; Lei, X.* “Studies towards the Synthesis of the Functionalized C3-C14 Decalin Framework of Alchivemycin A” Org. Chem. Front. 2016, 3, 251-258.
  105. Li, X.; Han, J.; Jones, A.; Lei, X.* “Chiral Boron Complex-Promoted Asymmetric Diels-Alder Cycloaddition and Its Application in Natural Product Synthesis” J. Org. Chem. 2016, 81, 458-468.
  106. 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).
  107. Dong, T.; Liao, D.; Liu, X.; Lei, X.* “Using Small Molecules to Dissect Non-apoptotic Programmed Cell Death” ChemBioChem 2015, 16, 2557-2561.
  108. 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.
  109. Li, T.; Liu, W.; Lu, S.; Zhang, Y-P.; Jia, L-M.; Chen, J.; Li, X.; Lei, X.; Dong, M.* “No Significant Increase in the Δ4- and Δ7-Dafachronic Acid Concentration in the Long-Lived glp-1 Mutant and in Dauer Formation-Defective Mutants” G3: Genes/Genomes/Genetics 2015, DOI: 10.1534/g3.115.018812
  110. Zhang, X.; Dong, T.; Li, Q.; Liu, X.; Li, L.; Chen, S.; Lei, X.* “Second-Generation TQ-Ligation for Cell Organelle Imaging” ACS Chem. Biol. 2015, 10, 1676-1683.
  111. Han, J.; Jones, A.; Lei, X.* “Recent Advances in the Total Synthesis of Prenylflavonoid and Related Diels-Alder Natural Products” Synthesis 2015, 47, 1519-1533.
  112. Dong, T.; Li, C.; Wang, X.; Dian, L.; Zhang, X.; Chen, X.; Li, L.; Cao, R.; Huang, N.; He, S. *; Lei, X.* “Ainsliadimer A selectively inhibits IKKα/β by covalently binding a conserved cysteine” Nature Commun. 2015, 6, 6522. (News story describing this work was highlighted in Chem. & Eng. News 2015, 15, 39).
  113. Liu, W.; Li, X.; Chen, J.; Li, T.; Dong, M.; Lei, X.* “Site-selective and Metal-free Aliphatic C-H Oxidation Enabled Synthesis of [5,24,25-D3]-(25S)-Δ7-Dafachronic acid” Chem. Eur. J. 2015, 21, 5345-5379
  114. 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)
  115. Du, M.; Lei, X.* Advanced in the synthesis of kaurane diterpe-noids. Youji Huaxue 2015, 35, 2447−2464
  116. Qin, X.; Chen, B.; Fu, J.; Shan, L.; Lei, X.; Zhang, W.* “Synthesis, cytotoxicity and inhibition of NO production of ivangustin enantiomer analogues” Eur. J. Med. Chem. 2015, 102, 256-265.
  117. Zhang, J.; Chen, J.; Zhang, X.; Lei, X.* “Total Syntheses of Menisporphine and Daurioxoisoporphine C Enabled by Photoredox-Catalyzed Direct C–H Arylation of Isoquinoline with Aryldiazonium Salt” J. Org. Chem. 2014, 79, 10682-10688
  118. Li, C.; Dong, T.; Li, Q.; Lei, X.* “Probing the Anti-cancer Mechanism of (-)-Ainsliatrimer A through Diverted Total Synthesis and Bioorthogonal Ligation” Angew. Chem. Int. Ed. 2014, 53, 12111-12115
  119. Zhang, J.; Wu, J.; Hong, B.; Ai, W.; Wang, X.; Li, H.; Lei, X.* “Diversity-oriented synthesis of Lycopodium alkaloids inspired by the hidden functional group pairing pattern” Nature Commun. 2014, 5, 4614
  120. 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
  121. Li, C.; Lei, X.* “Strategies toward the Biomimetic Syntheses of Oligomeric Sesquiterpenoids”    J. Org. Chem. 2014, 79, 3289-3295
  122. Liao, D.; Sun, L.; Liu, W.; He, S.; Wang, X.; Lei, X.* “Necrosulfonamide Inhibits Necroptosis by Selectively Targeting the Mixed Lineage Kinase Domain-like Protein” Med. Chem. Comm. 2014, 5, 333-337.
  123. Li, Q.; Dong, T.; Liu, X.; Zhang, X.; Yang, X.; Lei, X.* “ortho-Quinone Methide Finds Its Application in Bioorthogonal Ligation” Curr. Org. Chem. 2014, 18, 86-92.
  124. Li, T.; Chen, J.; Li, X.; Ding, X.; Wu, Y.; Zhao, L.; Chen, S.; Lei, X.*; Dong, M.* “Absolute Quantification of a Steroid Hormone that Regulates Development in Caenorhabditis elegans” Anal. Chem. 2013, 85, 9281-9287.
  125. Wang, X.; Li, H.; Lei, X.* “Challenges and Strategies to the Total Syntheses of Fawcettimine-Type and Serratinine-Type Lycopodium Alkaloids” Synlett. 2013, 24，1032-1043 (Invited Synpacts Article).
  126. 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).
  127. Li, C.; Dong, T.; Dian, L.; Zhang, W.; Lei, X.* “Biomimetic Syntheses and Structural Elucidation of the Apoptosis-Inducing Sesquiterpenoid Trimers: (-)-Ainsliatrimers A and B” Chem. Sci. 2013, 4, 1163-1167.
  128. 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).
  129. Huang, J.; Lei, X.* “A Nature-inspired Concise Synthesis of (+)-ent-Chromazonarol” Sci. China Chem. 2013, 56, 349-353.
  130. Li, H.; Wang, X.; Hong, B.; Lei, X.* “Collective Synthesis of Lycopodium Alkaloids and Tautomer Locking Strategy for the Total Synthesis of (-)-Lycojapodine A” J. Org. Chem. 2013, 78, 800-821. (Featured and Cover Article).
  131. Li, C.; Li, X.; Wang, X.; Lei, X.* “Diversity-Oriented Synthesis of Bicyclic Ring Systems via a Conjugate Addition/Aldol/RCM Process” Sci. China Chem. 2013, 56, 337-341.
  132. 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.
  133. Lei, X.*; Li, H. “Selective Alkene Metathesis in the Total Synthesis of Complex Natural Product” Top. Curr. Chem. 2012, 327, 163-196.
  134. 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).
  135. 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.
  136. Liao, D.; Li, H.; Lei, X.* “Efficient Generation of ortho-Quinone Methide: Application to the Biomimetic Syntheses of (±)-Schefflone and Tocopherol Trimers” Org. Lett. 2012, 14, 18-21.
  137. Li, C.; Tu, S.; Wen, S.; Li, S.; Chang, J.; Shao, F.; Lei, X.* “Total Synthesis of the G2/M DNA Damage Checkpoint Inhibitor Psilostachyin C” J. Org. Chem. 2011, 76, 3566-3570.
  138. Li, C.; Yu, X.; Lei, X.* “A Biomimetic Total Synthesis of (+)-Ainsliadimer A” Org. Lett. 2010, 12, 4284-4287.
  139. Gong, Y.; Wang, X.; Wang, J.; Yang, Z.; Li, S.; Yang, J.; Liu, L.; Lei, X.*; Shao, F. * “Chemical Probing Reveals Insights into the Signaling Mechanism of Inflammasome Activation” Cell Res. 2010, 20, 1289-1305.
  140. Han，Z.; Niu, T.; Chang, J.; Lei, X.; Zhao, M.; Wang, Q.; Cheng, W.; Wang, J.; Feng, Y.; Chai, J.* “Crystal structure of the FTO protein reveals basis for its substrate specificity” Nature 2010, 464, 1205-1209.

 

Prior to Independent Career

  1. Chou, T.; Dong, H.; Zhang, X.; Lei, X.; Hartung, J.; Zhang, Y.; Lee, H. L.; Wilson, R. M.; Danishefsky, S. J. * “Multifaceted Cytoprotection by Synthetic Polyacetylenes Inspired by the Ginseng-derived Natural Product Panaxytriol” Proc. Natl. Acad. Sci. USA 2011, 108, 14336-14341.
  2. Lee, L. S.; Stephenson,  K. K.;  Fahey, J. W.; Parsons, T. L.;  Lietman, P. S.;  Andrade, A. S.;  Lei, X. Yun, H.; Soon, G.H.; Shen, P.; Danishefsky, S. J.*; Flexner, C.* “Induction of Chemoprotective Phase 2 Enzymes by Ginseng and its Components” Planta Med. 2009; 75, 1129-1133
  3. Lei, X.; Danishefsky, S. J.* “Efficient Synthesis of a Novel Resorcyclide as Anticancer Agent Based on Hsp90 Inhibition” Adv. Synth. Catal. 2008, 350, 1677-1681
  4. Lei, X.; Dai, M.; Hua, Z.; Danishefsky, S. J.* “Biomimetic Total Synthesis of Tricycloillicinone and Mechanistic Studies Toward the Rearrangement of Prenyl Phenyl Ethers” Tetrahedron Lett. 2008, 49, 6383-6385
  5. Ng, F.; Yun, H.; Lei, X.; Danishefsky, S. J.; Fahey, J.; Stephenson, K.; Flexner, C.; Lee, L.* “(3R,9R,10R)-Panaxytriol: a molecular-based nutraceutical with possible application to cancer prevention and treatment” Tetrahedron Lett. 2008, 49, 7178-7179
  6. Peng, L. F.; Kim, S. S.; Matchacheep, S.; Lei, X.; Su, S.; Lin, W.; Runguphan, W.; Choe, W. H.; Sakamoto, N.; Beeler, A. B.; Porco, J. A., Jr.; Schreiber, S. L.* and Chung, R. T.* “Identification of Novel Epoxide Inhibitors of HCV Replication Using High-Throughput Screening.” Antimicrob. Agents Chemother. 2007, 51, 3756-3759.
  7. Lei, X.; Porco, J. A., Jr.* “Total Synthesis of the Diazobenzofluorene Antibiotic (-)-Kinamycin C.” J. Am. Chem. Soc. 2006, 128, 14790-14791. (News story describing this work was highlighted in Chem. & Eng. News 2006, 45, 9.)
  8. Porco, J. A., Jr.*; Su, S.; Lei, X.; Bardhan, S.; Rychnovsky, S. D. “Total Synthesis and Structure Assignment of (+)-Hexacyclinol” Angew. Chem. Int. Ed. 2006, 45, 5790-5792; Angew. Chem. 2006, 118, 5922-5924. (News stories describing this work were reported in Chem. & Eng. News 2006, 31, 11 and Nature 2006, 442, 492-493)
  9. Lei, X.; Zaarur, N.; Sherman, M. Y.; Porco, J. A., Jr.* “Stereocontrolled Synthesis of a Complex Chemical Library via Elaboration of Angular Epoxyquinol Scaffolds.” J. Org. Chem. 2005, 70, 6474-6483.
  10. Su, S.; Aquilano, D.; Arumugasamy, J.; Beeler, A. B.; Eastwood, E. L.; Giguere, J. R.; Lan, P.; Lei, X.; Min, G. K.; Yeager, A. R.; Zhou, Y.; Panek, J. S.; Snyder, J. K.; Schaus, S. E.; Porco, J. A., Jr.* “Convergent Synthesis of a Complex Oxime Library Using Chemical Domain Shuffling.” Org. Lett. 2005, 7, 2751-2754.
  11. Lei, X.; Porco, J. A., Jr.* “Synthesis of a Polymer-Supported Anthracene and Its Application as a Dienophile Scavenger.” Org. Lett. 2004, 6, 795-798.
  12. Lei, X.; Johnson, R. P.; Porco, J. A., Jr.* “Total Synthesis of the Ubiquitin-Activating Enzyme Inhibitor (+)-Panepophenanthrin.” Angew. Chem. Int. Ed. 2003, 42, 3913-3917; Angew. Chem. 2003, 115, 4043-4047. (This publication was highlighted as a “Hot Paper”.)

 

Patents

 

  1. Lei, X.; Li, Q.; Dong, T. CN 201611097411.2
  2. Lei, X.; Liao, D.; Yang, S. CN 201510574855.X
  3. Lei, X.; Liao, D.; Yang, S. CN 201510574855.X
  4. Lei, X.; He, S.; Li, C.; Dong, T. “Sesquiterpenoids” PCT/CN2014/076123
  5. Danishefsky, S. J.; Yun, H.; Chou, T.; Lei, X.; Sames, D. “Compounds and methods for treating cancer or neurotrophic disorder.” US2011/0124690
  6. Danishefsky, S. J.; Chou, T.; Lei, X.; Yun, H.; Ng, F.; Hartung, J.; Sames, D. “Compounds, compositions and methods for reducing toxicity and treating or preventing diseases.”    PCT Int. Appl. 2010, WO2010025272
  7. Danishefsky, S. J.; Chou, T.; Lei, X. “Compounds, compositions and methods for treating or preventing diseases.” PCT Int. Appl. 2009, WO2009105123
  8. Cottarel, G.; Gardner, T.; Lei, X.; Porco, J.; Schaus, S.; Wierzbowski, J. “Compositions and methods for potentiating antibiotic activity using an ATP receptor antagonist, coumarin, flavone, or terpene” PCT Int. Appl., 2008, WO2008019292
  9. Danishefsky, S. J. Lei, X.; Yun, H.; Chou, T. “Compositions and methods using a panaxytriol  compound in combination with a tubulin-binding drug for treating cancer or a neurotrophic disorder.”  PCT Int. Appl. 2008, WO 2008103916

Invited Lectures

 

  1. Tohoku University, 2018
  2. Tetrahedron Symposium, Italy, 2018
  3. University of Naples, 2018
  4. David Ginsburg Lecture, Technion-Israel Institute of Technology, 2018
  5. Weizmann Research Institute, 2018
  6. Tel Aviv University, 2018
  7. RACI National Centenary Conference, Melbourne, Australia, 2017
  8. Tetrahedron Symposium, Hungry, 2017
  9. Swiss Lecture Tour, Switzerland, 2017
  10. UCSF, 2017
  11. KAIST School of Molecular Science BK21 Symposium, South Korea, 2017
  12. CSJ Annual Conference, Tokyo, Japan, 2017
  13. ACBI Conference, Ho Chi Minh City, 2017
  14. ACP meeting in South Korea, 2016
  15. China-Thailand workshop on natural product and drug discovery, Thailand, 2016
  16. 27th European Colloquium of Heterocyclic Chemistry, Amsterdam, 2016
  17. 21st  iCeMS International Symposium“Emerging Science for Unlocking Cell's Secrets”, Kyoto, 2016
  18. RIKEN, Japan, 2016
  19. University of Tokyo, Japan, 2016
  20. Osaka University, Japan, 2016
  21. University of Hong Kong, 2016
  22. Hong Kong University of Science and Technology, 2016
  23. 9th Sino-German Frontiers of Science Symposium, Shenzhen, 2016
  24. University of California at Davis, USA, 2016
  25. IUPAC Congress, South Korea, 2015
  26. CSJ Symposium, Japan, 2015
  27. Sichuan University, 2015
  28. Chongqing University, 2015
  29. Xiamen University, 2014
  30. Sino-Japan Workshop on Chemical Biology, Beijing, 2014
  31. Gordon Research Conference on Heterocyclic Compounds, USA, 2014
  32. CGC Symposium on Chemical Biology by Max-Planck-Institute, Dortmund, 2014
  33. Keystone Conference on Cell Death, New Mexico, USA, 2014
  34. Asian Core Program Meeting on Chemical Biology, Philippines, 2014
  35. The Croucher Foundation Advanced Study Institute for Chemical Biology, Hong Kong, December 15-17, 2013
  36. National University of Singapore, 2013
  37. Nanyang Technological University, 2013
  38. The International Symposium on Natural Product Chemistry and Chemical Biology, Nagoya, Japan, November 20-23, 2013
  39. The Roche and RSC Chemistry Symposium: leading science for drug discovery, Shanghai, 2013
  40. ICBS 2013: The 2nd Annual Meeting of the International Chemical Biology Society in Kyoto, Japan, 2013
  41. The first Asian conference for “MONODUKURI” Strategy by Synthetic Organic Chemistry (ACMS) in Okinawa, Japan, 2013
  42. Tsinghua University, 2013
  43. Nankai University, 2013
  44. 3rd Annual Chemical BiologySymposium of our Synthetic and Functional Biomolecules Center (SFBC) at Peking University, 2013
  45. “Gao Ji Yu Lecture” Nanjing University, 2013
  46. East China Normal University, 2013
  47. China Pharmaceutical University, 2013
  48. The 7th International Conference on Cutting-Edge Organic Chemistry in Asia, Singapore, 2012
  49. The 4th China-Thailand Workshop on Natural Products and Drug Discovery, Songkla, Thailand, 2012
  50. International Conference of Chemical Biology of Natural Products: Target ID and Regulation of Bioactivity, Kyoto, Japan, 2012
  51. International Symposium on Natural Product Synthesis and Innovative Process Methods for Drug Manufacture, Chongqing, China, 2012
  52. Cell Symposium: Genetics & Chemistry, Boston, USA, 2012
  53. 8th Sino-US Chemistry Professor Conference, Kunming, China, 2012
  54. National Meeting of Chinese Chemistry Society, Chengdu, China, 2012
  55. Oriental Scientific Symposium on Organic Synthesis, Shanghai, China, 2012
  56. National Organic Symposium of China, Nanjing, China, 2011
  57. Lanzhou University, Lanzhou, China, 2011
  58. Second Military Medical University, Shanghai, China, 2011
  59. Nankai University, Tianjin, China, 2011
  60. Pacifichem Congress, Honolulu, December 20th, 2010
  61. ACS National Meeting, Boston, USA, 2010
  62. ESF-COST Conference on Natural Products Chemistry, Biology and Medicine III, Acquafredda di Maratea, Italy, 2010
  63. Peking University, Beijing, China, 2010
  64. 6th Sino-US Chemistry Professor Conference, Hangzhou, China, 2010
  65. 5th Sino-US Chemistry Professor Conference, Lanzhou, China, 2009

 

Grants

 

  • NNSFC-Distinguished Young Investigator (21625201), 2017-2021, PI
  • NNSFC (21561142002), 2015-2018, PI
  • National High Technology Projects 973 (2015CB856200), 2015-2019, Co-PI
  • NNSFC (21472010), 2015-2017, PI
  • NNSFC (91313303), 2014-2015, Co-PI
  • National High Technology Projects 973 (2012CB837400), 2012-2016, Chief Scientist
  • NNSFC-Outstanding Young Investigator (20122209), 2013-2015, PI
  • NNSFC (21072150), 2011-2013, PI
  • Program for New Century Excellent Talents in University (NCET-10-0614), 2011-2013, PI
  • National High Technology Projects 863 (2008AA022317), 2009-2011, PI
  • NNSFC (20802050), 2009-2011, PI

 

Teaching

 

  • 2014-, “Introduction to Chemical Biology” for undergraduate students, Peking University
  • 2014-, “Organic Chemistry” for undergraduate students, Peking University
  • 2012-, PTN program “Chemical Biology”
  • 2009-2012, Tianjin University “Medicinal Chemistry” for graduate students
  • 2009-2012, Tianjin University “Advanced Organic Chemistry” for undergraduate students