Research Experience
2017-now: Peking University College of Chemistry
2014-now: Peking-Tsinghua Center for Life Sciences
2014-2017: Peking University College of Chemistry
2013-2014: National Institute of Biological Science (NIBS)
2008-2012: National Institute of Biological Science (NIBS)
2008-2013: Tianjin University School of Pharmaceutical Science
2006-2008: Columbia University
2001-2006: Ph.D. (Organic Synthesis), Boston University, Supervisor: Prof. John Porco
1997-2001: B.S. (Chemistry), Peking University, Supervisor: Prof. Jianbo Wang
Awards
David Ginsburg Memorial Lectureship Award, 2018
CCS-BASF Young Investigator Award, 2018
Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017
Swiss Chemical Society Distinguished Lectureship Award, 2017
KAIST School of Molecular Science Lectureship Award, 2017
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 Chinese Young Investigator Award, 2014
National Leading Young Scientific Investigator Award, 2013
Chinese Chemical Society Prize for Young Scientists, 2013
Young Chemical Biologist Award by the International Chemical Biology Society (ICBS), 2013
Servier Young Investigator Award by Chinese Pharmaceutical Association, 2013
Thieme Chemistry Journal Award, 2013
Asian Core Program Lectureship Award, 2012
Outstanding Young Investigator Award by National Natural Science Foundation of China, 2012
New Century Excellent Talents in University Award, 2010
WuXi PharmaTech 2010 Life Science and Chemistry Award, 2010
IUPAC Young Chemist Award, 2009
NESACS-JCF/GDCh Exchange Scholarship to Germany, 2005
Travel Award for the Gordon Research Conference on Combinatorial Chemistry, 2005
Sugata Ray Memorial Award for Excellence in Research and Teaching at Boston University, 2005
Research Interests
Chemical Biology, Natural Product Synthesis, Synthetic Biology, Drug Discovery
- Using small molecules probes to dissecting fundamental cellular processes, such as programmed cell death
- Using a combined efforts of synthetic chemistry and synthetic biology to prepare complex natural products with significant biological functions
- Developing new chemical biology tools to explore complex protein structures and protein-protein interactions
- Developing the first-in-class drug candidates for the treatment of cancers, infectious diseases and auto-immune diseases
Selected Publications
- 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, doi: 10.1038/s41557-020-0467-7
- 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, doi: 10.1021/acscatal.0c01187
- 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, doi: 10.1021/acscentsci.0c00122
- 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
- Hong, B.; Luo, T.; Lei, X.* “Late-Stage Diversification of Natural Products” ACS Cent. Sci. 2020, doi:10.1021/acscentsci.9b00916
- Bai, Y.; Lam, H.C.; Lei, X.* “Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, doi: 10.1021/acs.accounts.9b00600
- 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, S0168-8278 (20) 30124-0
- 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
- 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.
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- Yaocheng Shi, Zhi Xu, Renxiang Tan, Xiaoguang Lei* “Divergent Total Synthesis of Chaetoglines C to F” J. Org. Chem. 2019, 84, 8766-8770
- 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)
- Jinbao Wu, Yuichiro Kadonaga, Benke Hong, Jin Wang, Xiaoguang Lei* “Enantioselective Total Synthesis of (+)-Jungermatrobrunin A” Angew. Chem. Int. Ed. 2019, 58, 10879-10883
- 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
- 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
- Wang X, Du C, Hong B, Lei X.* “Total synthesis of (±)-antroquinonol”. Org. Biomol. Chem. 2018, 17, 1754-1757.
- Xiao F, Zhang X, Lei X.* “Recent Developments and Applications of Photoconjugation Chemistry”. Chimia 2018, 72, 782-790
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- Li, H.; Lei, X.* “Fawcettimine-Type Lycopodium Alkaloids as a Driving Force for Discoveries in Organic Synthesis” Chem. Rec. 2018, 18, 543-554
- 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.
- 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.
- 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.
- 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.
- 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)
- Zhuang, S.; Li, Q.; Cai, L.; Wang, C.*; Lei, X.* “Chemoproteomic Profiling of Bile Acid Interacting Proteins” ACS Cent. Sci. 2017, 3, 501-509.
- Jones, A.; Zhang, X.; Lei, X.* “Covalent Probe Finds Carboxylic Acid” Cell Chem. Biol. 2017, 24, 537-538.
- 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.
- 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.
- 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.
- 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).
- Li, C.; Jones, A.; Lei, X.* “Synthesis and Mode of Action of Oligomeric Sesquiterpene Lactones” Nat. Prod. Rep. 2016, 33, 602-611. (Cover story)
- 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.
- Liao, D.; Yang, S.; Wang, J.; Zhang, J. Hong, B.; Wu, F.; Lei, X.* “Total Synthesis and Structural Reassignment of Aspergillomarasmine A” Angew. Chem. Int. Ed. 2016, 55, 4291-4295.
- Liu, W.; Li, H.; Cai, P.; Wang, Z.; Yu, Z-X.; Lei, X.* “Scalable Total Synthesis of Jungermannenones B and C” Angew. Chem. Int. Ed. 2016, 55, 3112-3116. (Highlighted by Synfacts 2016, 12, 0332).
- 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).
- Gao, L.; Han, J.; Lei, X.* “Enantioselective Total Syntheses of Kuwanon X, Kuwanon Y and Kuwanol A” Org. Lett. 2016, 18, 360-363.
- 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.
- 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.
- 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.
- 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.
- 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).
- Dong, T.; Liao, D.; Liu, X.; Lei, X.* “Using Small Molecules to Dissect Non-apoptotic Programmed Cell Death” ChemBioChem 2015, 16, 2557-2561.
- 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.
- 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
- 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.
- 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.
- 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).
- 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
- 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)
- 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.
- 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
- 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
- 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
- Han, J.; Li, X.; Guan, Y.; Zhao, W.; Wullf, W. D.*; Lei, X.* “Enantioselective Biomimetic Total Syntheses of Kuwanons I and J and Brosimones A and B” Angew. Chem. Int. Ed. 2014, 53, 9257-9261
- Li, C.; Lei, X.* “Strategies toward the Biomimetic Syntheses of Oligomeric Sesquiterpenoids” J. Org. Chem. 2014, 79, 3289-3295
- 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.
- 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.
- 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.
- 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).
- 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).
- 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.
- 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).
- Huang, J.; Lei, X.* “A Nature-inspired Concise Synthesis of (+)-ent-Chromazonarol” Sci. China Chem. 2013, 56, 349-353.
- 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).
- 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.
- 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.
- Lei, X.*; Li, H. “Selective Alkene Metathesis in the Total Synthesis of Complex Natural Product” Top. Curr. Chem. 2012, 327, 163-196.
- 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).
- 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.
- 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.
- 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.
- Li, C.; Yu, X.; Lei, X.* “A Biomimetic Total Synthesis of (+)-Ainsliadimer A” Org. Lett.2010, 12, 4284-4287.
- 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.
- 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
- 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.
- 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
- 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
- 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
- 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
- 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.
- 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.)
- 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)
- 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.
- 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.
- 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.
- 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”.)
