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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 C518, 
     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 – now Boya Distinguished Professor, College of Chemistry and Molecular Engineering, Peking University, China
2021 – now Senior Principal Investigator, Institute for Cancer Research, Shen Zhen Bay Laboratory, 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

 

Honors and 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, 2021Cheung 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

 

Affiliation

 

Scientific Founder of HepaiTech Biopharm Inc.
Scientific Founder of Iongen Therapeutics Inc.
Scientific Founder of ReadCrystal Inc.Adjunct Professor of Chulalongkorn University, Thailand
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

Associate Editor, JACS Au, 2025-
Editor, Bioorganic and Medicinal Chemistry, 2017-2025
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 and translational medicine
Natural product total synthesis and biosynthesis
Synthetic biology and biocatalysis
Medicinal chemistry and drug discovery

 

 

Publications1. Xiaojiao Guo, Lei Gao, Shiwei Li, Jing Gao, Yuanyuan Wang, Jing Lv, Jiayi Wei, Jing Yang,

  1. Han Ke, Qi Ding, Jun Yang, Fusheng Guo, Haowen Zhang, Xiaoguang Lei*, Le Kang* “Decoding 4-vinylanisole biosynthesis and pivotal enzymes in locusts” Nature 2025, accepted
  2. Jing-Yang He, Caiping Tian, Qiang Li, Jian Zhang, Ji-Xiang He, Lingqiang Zhang, Xiaoguang Lei*, Jing Yang* “Proteolysis-assisted cyclization facilitates site-centric target deconvolution of isothiocyanates” Nature Chem. Biol. 2025, in revision
  3. 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)
  4. Fusheng Guo, Jing Zhang, Yihui Gao, Zhou Shu, Fei Sun, Jing Ma, Xu Zhou, Wenyang Li, Huawei Mao*, Xiaoguang Lei* “Discovery and Total Synthesis of Anhydrotuberosin as a STING Antagonist for Treating Autoimmune Diseases” Angew. Chem. Int. Ed. 2025, 64, e202407641
  5. Junping Fan*, Wenjun Xie, Han Ke, Jing Zhang, Jin Wang, Haijun Wang, Nianxin Guo, Yingjie Bai, Xiaoguang Lei* “Structural Basis for Inhibition of Urate Reabsorption in URAT1” JACS Au, 2025, 5, 1308–1319
  6. Jiawen Wu, Fusheng Guo, Chenju Yi, Rongjie Yang, Xiaoguang Lei, Zhonghua Xia* “Photosensitized Gold-Catalyzed Cross-Couplings of Aryl Bromides” J. Am. Chem. Soc. 2025, 147, 5839–5850
  7.  Yi Yang, Ling Jiao, Fusheng Guo, Yibin Sun, Hongyang Cui, Xiaoguang Lei, Jianying Hu, Yi Wan* “Protein-Affinity Guided Nontargeted Analysis Reveals the Widespread FXR-Antagonistic Pollutants in Surface Water and Source Water Along the Yangtze River and Yellow River” Environ. Sci. Technol. 2025, 59, 2368–2377
  8. 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)
  9.  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
  10. Jin Wang, Jianxiong Zhao, Zhenyang Yu, Siyuan Wang, Fusheng Guo, Jun Yang, Lei Gao, Xiaoguang Lei* “Concise and Modular Chemoenzymatic Total Synthesis of Bisbenzylisoquinoline Alkaloids” Angew. Chem. Int. Ed. 2024, 63, e202414340
  11. Fusheng Guo, Fan Xiao, Hao Song, Xiaoyong Li, Yaxin Xiao, Yong Qin*, Xiaoguang Lei* “An optimized marinopyrrole A derivative targets GlmS to inhibit MRSA” ACS Cent. Sci. 2024, doi.org/10.1021/acscentsci.4c01167
  12.  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)
  13. Lei Gao, Qi Ding, Xiaoguang Lei* “Hunting for the intermolecular Diels-Alderase” Acc. Chem. Res. 2024, 57, 2166–2183 (Cover article)
  14. Shunkang Wu, Yuelin Deng, Haobo Sun, Xuewen Liu, Shuo Zhou, Hanxi Zhao, Huan Li, Fusheng Guo, Qiuyu Yue, Fan Wu, Xiao-Jun Huang, Xiaoguang Lei, Xiangmin Tong, Xiaofei Gao, Hsiang-Ying Lee* “BRAF inhibitors enhance erythropoiesis and treat anemia through paradoxical activation of MAPK signaling” Sig. Trans. and Targ. Ther. 2024, 9, 338
  15. Xiaofan Ding, Mengxue Sun, Fusheng Gu, Xinmin Qia, Haoyu Yuan, Wenjiao Lou, Qixuan Wang, Xiaoguang Lei*, Wenwen Zeng* “Picrasidine S induces cGAS-mediated cellular immune response as a novel vaccine adjuvant” Adv. Sci. 2024, 11, e2310108
  16.  Zixin Feng, Fu-sheng Guo, Qian Wang, Miao Wang, Ming-Hui Zhao, Zhao Cui*, Xiaoguang Lei* “Macrocarpal B blocks the binding between the phospholipase A2 receptor and its antibodies” Bioorg. Med. Chem. 2024, 110, 117793
  17. Haoran Dong, Xiaoguang Lei* “Synthesis of (+)-epicolidine C and the 6/6/6/5 tetracyclic core of spylidone” Tetrahedron Letters, 2024, 146, 155181
  18. Junping Fan*, Han Ke, Jing Lei, Jin Wang, Makoto Tominag, and Xiaoguang Lei* “Structural basis of TRPV1 inhibition by SAF312 and cholesterol” Nature Communications 2024, 15, 6689
  19. Junxiu Nong, Shengqiang Shen, Fan Hong, Fan Xiao, Lingtian Meng, Pilong Li, Xiaoguang Lei*, Ye-Guang Chen* “Verteporfin inhibits TGF-β signaling by disrupting the Smad2/3-Smad4 interaction” Mol. Bol. Cell 2024, 35, ar95
  20. Haowen Zhang, Shuhan Xie, Jun Yang, Ning Ye, Feng Gao, Fabrice Gallous, Lei Gao,* and Xiaoguang Lei* “Chemoenzymatic Synthesis of 2-Aryl Thiazolines from 4- Hydroxybenzaldehydes Using Vanillyl Alcohol Oxidases” Angew. Chem. Int. Ed. 2024, 63, e202405833
  21. 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)
  22. Junping Fan*, Chang Guo, Daohong Liao, Han Ke, Jing Lei, Wenjun Xie, Yuliang Tang, Makoto Tominaga, Zhuo Huang*, Xiaoguang Lei* “Structural Pharmacology of TRPV4 Antagonists” Adv. Sci. 2024, 11, e2401583
  23. Qi Ding, Nianxin Guo, Lei Gao*, Michelle McKe, Dongshan Wu, Jun Yang, Junping Fan, JingKe Weng, Xiaoguang Lei* “The evolutionary origin of naturally occurring intermolecular DielsAlderases from Morus albaNature Communications 2024, 15, 2492.
  24. 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 2024, 4, 619-634
  25. Yihui Gao, Mingzhe Ma, Wenyang Li,* and Xiaoguang Lei* “Chemoproteomics, A Broad Avenue to Target Deconvolution” Adv. Sci. 2024, 11, 2305608
  26. Jiaming Yu, Hui Guo, Jing Zhang, Jiansen Hu, Hongtao He, Caixia Chen, Na Yang, Fan Yang, Zexu Lin, Huanqin Dai, Liming Ouyang, Cuihua Liu, Xiaoguang Lei, Lixin Zhang, Guoliang Zhu*, Fuhang Song* “Chrysomycins, Anti-Tuberculosis C-Glycoside Polyketides from Streptomyces sp. MS751” Marine Drugs 2024, 22, 259
  27. 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
  28. Qixuan Wang, Fusheng Guo, Jin Wang, Xiaoguang Lei* “Divergent Total Syntheses of ITHQtype Bis-β-carboline Alkaloids by Regio-selective Formal Aza-[4+2] Cycloaddition and Late
    stage C-H Functionalization” Chem. Sci. 2023, 14, 10353-1035929.
  29. Sanshan Wang, Kaiqi Chen, Fusheng Guo, Wenneng Zhu, Chendi Liu, Haoran Dong, Jin-Quan Yu*, Xiaoguang Lei* “C–H Glycosylation of Native Carboxylic Acids: Discovery of Antidiabetic SGLT-2 Inhibitors” ACS Cent. Sci. 2023, 9, 1129–1139
  30. Haoran Dong, Dachao Hu, Benke Hong, Jin Wang, Xiaoguang Lei* “Total Syntheses of Diverse Tetramic Acid-Bearing cis-Decalin Natural Products” Angew. Chem. Int. Ed. 2023, 62,
    e202301872
  31. 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, 992- 1007
  32. Peiqi Chen, Qiang Li*, Xiaoguang Lei* “Review of the impact of fragment-based drug design on PROTAC degrader discovery” Trends in Analytical Chemistry 2024, 171, 117539
  33. 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
  34. 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
  35. 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
  36. 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
  37.  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, 2, 2830–2838
  38. Fusheng Guo, Yihui Gao, Xiaobao Li*, Xiaoguang Lei* “Natural Product 2-Oxokolavenol Is a Novel FXR Agonist” Molecules 2022, 27, 896839.
  39. 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
  40. 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
  41. Mengyue Deng, Yue Li, Yulu Li, Xiaolan Mao, Han Ke , Weiling Liang , Xiaoguang Lei, YuLung Lau, Huawei Mao* “A Novel STAT3 Gain-of-Function Mutation in Fatal Infancy-Onset Interstitial Lung Disease” Front. Immunol. 2022,13, 866638
  42. 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
  43.  Dongshan Wu, Xiaoguang Lei* “Enzymatic cascade reactions for the efficient synthesis of natural products” Tetrahedron 2022, 127, 133099
  44. 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.
  45. 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
  46. Yange Niu, Wenhao Cui, Rui Liu, Sanshan Wang, Han Ke, Xiaoguang Lei, Lei Chen* “Structural mechanism of SGLT1 inhibitors” Nature Commun. 2022, 13, 6440  
  47. 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
  48. Lei Gao, Jun Yang, Xiaoguang Lei* “Enzymatic intermolecular Diels-Alder reactions in synthesis: From nature to design” Tetrahedron Chem 2022, 2, 100013
  49. 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, 545-55850.
  50. 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
  51. 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.
  52. 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, 9, nwac046
  53. 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
  54. 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
  55. 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.
  56. 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
  57. 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- 916.58.
  58. 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
  59.  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
  60.  Bai Y, Zhang L, Lei X* “Human Endogenous Natural Products” Prog. Chem. Org. Nat. Prod. 2021, 114, 313-337.
  61. 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.
  62. 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
  63. Lei Gao*, Xiaoguang Lei* “Biosynthetic Intermediate Probes for Visualizing and Identifying the Biosynthetic Enzymes of Plant Metabolites” ChemBioChem 2021, 22, 982-984
  64. 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
  65. 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 aeruginosaCCS Chemistry 2020, 2, 2405-2417
  66. 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
  67. 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
  68.  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
  69. 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)
  70. 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
  71. 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
  72. 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
  73. Hong, B.; Luo, T.; Lei, X.* “Late-Stage Diversification of Natural Products” ACS Cent. Sci. 2020, 6, 622-635
  74. Bai, Y.; Lam, H.C.; Lei, X.* “Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, 53, 1034-1045
  75. 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
  76. 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
  77. Wang J, Hong B, Hu D, Kadonaga Y, Tang R, Lei X.* “Protecting-Group-Free Syntheses of entKaurane Diterpenoids: [3+2+1] Cycloaddition/Cycloalkenylation Approach.” J. Am. Chem. Soc. 2020, 142, 2238-2243.
  78.  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
  79.  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, 4115-412080.
  80. 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
  81. 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
  82. 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
  83. 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
  84. Alexander X. Jones, Yong Cao, Yu-Liang Tang, Jian-Hua Wang, Yue-He Ding, Hui Tan, ZhenLin 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
  85. 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 aeruginosaChem. Sci. 2019, 10, 6635-6641
  86. Yaocheng Shi, Zhi Xu, Renxiang Tan, Xiaoguang Lei* “Divergent Total Synthesis of Chaetoglines C to F” J. Org. Chem. 2019, 84, 8766-8770
  87. 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)
  88. Jinbao Wu, Yuichiro Kadonaga, Benke Hong, Jin Wang, Xiaoguang Lei* “Enantioselective Total Synthesis of (+)-Jungermatrobrunin A” Angew. Chem. Int. Ed. 2019, 58, 10879-10883
  89. 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. 201972461-468
  90. Chen, K.; Lei, X.* Recent applications of C-H functionalization in complex molecule synthesis. Curr. Opin. Green Sustain. Chem. 2018, 11, 9-14
  91. 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
  92. Wang X, Du C, Hong B, Lei X.* “Total synthesis of (±)-antroquinonol”. Org. Biomol. Chem. 2018, 17, 1754-1757.
  93. Xiao F, Zhang X, Lei X.* “Recent Developments and Applications of Photoconjugation Chemistry”. Chimia 2018, 72, 782-790
  94. 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
  95. 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
  96. 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
  97. 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
  98. 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- 743699.
  99. 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
  100. Yue, Z.; Xiao, X.; Wu, J.; Zhou, X.; Liu, W.; Liu, Y.; Li, H.; Chen, G.; Wu, Y.*; Lei, X.* entJungermannenone C Triggers Reactive Oxygen Species-Dependent Cell Differentiation in Leukemia Cells” J. Nat. Prod. 2018, 81, 298-306
  101. 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
  102. Li, H.; Lei, X.* “Fawcettimine-Type Lycopodium Alkaloids as a Driving Force for Discoveries in Organic Synthesis” Chem. Rec. 2018, 18, 543-554
  103. 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.
  104. 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.
  105. 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.
  106. 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.
  107.  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)
  108. Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509.
  109. Jones, A.; Zhang, X.; Lei, X.* “Covalent Probe Finds Carboxylic Acid” Cell Chem. Biol. 2017, 24, 537-538.
  110. 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.
  111. 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.
  112. 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.
  113. 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).
  114. Li, C.; Jones, A.; Lei, X.* “Synthesis and Mode of Action of Oligomeric Sesquiterpene Lactones” Nat. Prod. Rep. 2016, 33, 602-611. (Cover story)
  115. 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.
  116. 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.
  117.  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).
  118. 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).
  119. Gao, L.; Han, J.; Lei, X.* “Enantioselective Total Syntheses of Kuwanon X, Kuwanon Y and Kuwanol A” Org. Lett. 2016, 18, 360-363.
  120. 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
  121. 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.
  122. 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.
  123. 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.
  124. 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).
  125. Dong, T.; Liao, D.; Liu, X.; Lei, X.* “Using Small Molecules to Dissect Non-apoptotic Programmed Cell Death” ChemBioChem 2015, 16, 2557-2561.
  126. 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.
  127. 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
  128. Zhang, X.; Dong, T.; Li, Q.; Liu, X.; Li, L.; Chen, S.; Lei, X.* “Second-Generation TQLigation for Cell Organelle Imaging” ACS Chem. Biol. 2015, 10, 1676-1683.
  129.  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.
  130. 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).
  131.  Liu, W.; Li, X.; Chen, J.; Li, T.; Dong, M.; Lei, X.* “Site-selective and Metal-free Aliphatic CH Oxidation Enabled Synthesis of [5,24,25-D3]-(25S)-Δ 7 -Dafachronic acid” Chem. Eur. J. 2015, 21, 5345-5379132.
  132. 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)
  133. Du, M.; Lei, X.* Advanced in the synthesis of kaurane diterpe-noids. Youji Huaxue 2015, 35, 2447−2464
  134. 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.
  135. 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
  136. 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
  137. 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
  138. 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
  139.  Li, C.; Lei, X.* “Strategies toward the Biomimetic Syntheses of Oligomeric Sesquiterpenoids” J. Org. Chem. 2014, 79, 3289-3295
  140.  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.
  141.  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.
  142.  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 elegansAnal. Chem. 2013, 85, 9281-9287.
  143. Wang, X.; Li, H.; Lei, X.* “Challenges and Strategies to the Total Syntheses of FawcettimineType and Serratinine-Type Lycopodium Alkaloids” Synlett. 2013, 241032-1043 (Invited Synpacts Article).
  144.  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).
  145. 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.
  146.  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).
  147. Huang, J.; Lei, X.* “A Nature-inspired Concise Synthesis of (+)-ent-Chromazonarol” Sci. China Chem. 2013, 56, 349-353.
  148. 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).
  149.  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.
  150. 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.
  151. Lei, X.*; Li, H. “Selective Alkene Metathesis in the Total Synthesis of Complex Natural Product” Top. Curr. Chem. 2012, 327, 163-196.
  152. 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).
  153.  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.
  154. 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, 18-21.155.
  155. 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.
  156. Li, C.; Yu, X.; Lei, X.* “A Biomimetic Total Synthesis of (+)-Ainsliadimer A” Org. Lett. 2010, 12, 4284-4287.
  157. 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.
  158.  HanZ.; 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
  159. 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.
  160.  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
  161.  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
  162.  Lei, X.; Dai, M.; Hua, Z.; Danishefsky, S. J.* “Biomimetic Total Synthesis of Tricycloillicinone and Mechanistic Studies Toward the Rearrangement of Prenyl Phenyl Ethers”
    etrahedron Lett. 2008, 49, 6383-6385
  163. 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
  164. 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, 3756-3759.165.
  165. 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.)
  166. 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)
  167.  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.
  168. 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.
  169. 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.
  170. 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
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