生物医药

化学生物学，天然产物合成，合成生物学，创新药物研发

Total Synthesis;Natural Products;Diabetes;Insulin Resistance;Metabolic Dysfunctions;Obesity;Inflammation;Liver;NASH;Macrophage

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 & Microbe2020,27, 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”Phytochemistry2020,71, 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 Acta2019,1102, 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*, andXiaoguang Lei*“Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression”Proc. Natl Acad. Sci. USA2019,116, 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”eLife2019,8, 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 novosynthesis, structural assignment and biological evaluation of pseudopaline, a metallophore produced byPseudomonas 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”Chem2019,6,1671-1681 (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”.Chimia2018, 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”.elife2018, 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”eLife2016; 5:e12509. (News story describing this work was highlighted byNature Methods2016,13, 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 bySynfacts2016,12, 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 byChem. & Eng. News2015,93, 35 andSynfacts2015,11, 1231).
Dong, T.; Liao, D.; Liu, X.;Lei, X.*“Using Small Molecules to Dissect Non-apoptotic Programmed Cell Death”ChemBioChem2015,16, 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”Science2015,349, 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/Genetics2015, 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 ofPrenylflavonoid and Related Diels-Alder Natural Products”Synthesis2015,47, 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 inChem. & Eng. News2015,15, 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 bySynfacts2015,11, 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 ofLycopodiumalkaloids 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 inCaenorhabditis 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 inChem. & Eng. News2013,14, 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 inChem. & Eng. News2013,2, 37;Nature Asia2012, 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 ofLycopodiumAlkaloids 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”Cell2012,148, 213-227. (News stories describing this work were highlighted inChem. & Eng. News2012,5, 40;Nature China2012, February 1;Asian Scientist2012, January31; andNature Reviews Molecular Cell Biology, 2012,Feb. 8).
Li, H.; Wang, X.;Lei, X.*“Total Syntheses ofLycopodiumAlkaloids (+)-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”Nature2010, 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. USA2011,108, 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 inChem. & Eng. News2006,45, 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 inChem. & Eng. News2006,31, 11 andNature2006,442, 492-493)
Lei, X.; Zaarur, N.; Sherman, M. Y.; Porco, J. A., Jr.*“Stereocontrolled Synthesis of a Complex Chemical LibraryviaElaboration 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”.)

1. 化合物、组合物及其方法
海湃泰克（北京）生物医药科技有限公司
沈瑞超; 雷晓光; 汪晓明; 李毓龙; 何若愚
公开日期: 2025-06-10 申请日期: 2023-10-20 公开号: CN120129676A

2. 氧杂环丁烷合成酶突变体及其应用
北京大学
雷晓光; 高磊; 王海军; 柯翰
公开日期: 2025-03-21 申请日期: 2024-11-04 公开号: CN119662618A

3. COMPOUNDS AND METHOD OF USE THEREOF FOR TREATING BACTERIAL DISEASES
PEKING UNIVERSITY; INSTITUTE OF GENETICS AND DEVELOPENTAL BIOLOGY CHINESE ACADEMY OF SCIENCES
Xiaoguang LEI; Jian-Min Zhou; Haijun Wang; Pei Miao; Wei Wang
公开日期: 2025-01-16 申请日期: 2024-06-06 公开号: US20250019341A1

4. 苯并杂环类化合物、其药学上可接受的盐或立体异构体及其制备方法与应用
江苏集萃分子工程研究院有限公司
雷晓光; 张静; 郭富生
公开日期: 2025-01-14 申请日期: 2023-07-14 公开号: CN119306737A

5. 多环化合物及其方法
海湃泰克（北京）生物医药科技有限公司
雷晓光; 汪晓明; 李毓龙
公开日期: 2024-09-17 申请日期: 2022-11-14 公开号: CN118660883A

6. 一种基于香草醇氧化酶的含氮杂环化合物的合成方法
北京大学
雷晓光; 高磊; 张浩文
公开日期: 2024-08-16 申请日期: 2024-04-18 公开号: CN118497159A

7. 用于治疗细菌性疾病的化合物及其使用方法
北京大学; 中国科学院遗传与发育生物学研究所
雷晓光; 周俭民; 王海军; 缪佩; 王伟
公开日期: 2024-08-16 申请日期: 2022-12-06 公开号: CN118510752A

8. 作为PU.1抑制剂的化合物
浙江星浩澎博医药有限公司
王鑫; 吴虹; 郭富生; 雷晓光; 姚宁宁
公开日期: 2023-12-08 申请日期: 2021-11-18 公开号: CN117203198A

9. 特异性表达hMRGPRX2的转基因小鼠的构建方法及其应用
海湃泰克（北京）生物医药科技有限公司
刘英骏; 汪晓明; 沈瑞超; 李毓龙; 雷晓光; 马强; 刘卓; 闫培丽
公开日期: 2023-09-29 申请日期: 2023-06-30 公开号: CN116814689A

10. COMPOUNDS AS PU. 1 INHIBITORS
S-Infinity Pharmceuticals
LEI Xiaoguang; WU Hong; WANG Xin; YAO Ningning; GUO Fusheng
公开日期: 2023-09-27 申请日期: 2021-11-18 公开号: EP4247805A1

11. 泰妙菌素在制备用于治疗银屑病的药物中的应用
中国医学科学院皮肤病医院（中国医学科学院皮肤病研究所）
向睿宇; 杨勇; 胡凌寒; 雷晓光
公开日期: 2023-08-18 申请日期: 2022-02-23 公开号: CN114366732B

12. 一种红树内生真菌中二萜类化合物及其制备方法和应用
海南师范大学
陈光英; 覃玉月; 黎婉珊; 雷晓光; 李小宝; 魏艳梅
公开日期: 2023-04-04 申请日期: 2021-09-30 公开号: CN115894514A

13. 一种Diels-Alder反应酶突变体及其制备方法与应用
北京大学
雷晓光; 王进; 高磊
公开日期: 2023-03-21 申请日期: 2022-10-25 公开号: CN115820576A

14. 复方吉西他滨组合物及应用
江苏集萃分子工程研究院有限公司
雷晓光; 汪晓明; 廖道红; 黄道飞; 张秀国
公开日期: 2023-01-10 申请日期: 2022-11-25 公开号: CN115581703A

15. 蝙蝠葛生物碱类化合物在治疗代谢性疾病中的应用
北京大学第三医院（北京大学第三临床医学院）
雷晓光; 姜长涛; 张志威; 汪锴; 乔杰
公开日期: 2022-11-18 申请日期: 2022-05-07 公开号: CN114569613B

16. 细胞坏死抑制剂
北京生命科学研究所
张志远; 王晓东; 雷晓光; 苏亚宁; 何苏丹; 阮寒英; 孙丽明
公开日期: 2022-10-18 申请日期: 2015-12-23 公开号: CN115197098A

17. 一种新型疫苗佐剂及其用途
清华大学; 北京大学
曾文文; 雷晓光; 丁晓凡; 郭富生
公开日期: 2022-10-11 申请日期: 2022-06-28 公开号: CN115154597A

18. 细胞坏死抑制剂
北京生命科学研究所
王晓东; 何苏丹; 阮寒英; 张志远; 雷晓光; 苏亚宁; 孙丽明
公开日期: 2022-08-19 申请日期: 2015-12-23 公开号: CN107108467B

19. 亚胺还原酶突变体M5及其在合成氮杂环手性胺中的应用
江苏集萃分子工程研究院有限公司
廖道红; 高书山; 雷晓光; 张军
公开日期: 2022-07-08 申请日期: 2022-03-23 公开号: CN114717211A

20. 蝙蝠葛生物碱类化合物在治疗代谢性疾病中的应用
北京大学第三医院（北京大学第三临床医学院）
雷晓光; 姜长涛; 张志威; 汪锴; 乔杰
公开日期: 2022-06-03 申请日期: 2022-05-07 公开号: CN114569613A

1. 新型生物正交反应的研究及应用
立项时间: 2015-2018 项目经费：950000

2. 调控细胞死亡的复杂天然产物的发现，合成与化学生物学研究
立项时间: 2015-2018 项目经费：2520000

3. 天然产物全合成与前沿化学生物学研究
立项时间: 2013-2015 项目经费：1000000

4. DNA损伤反应引起的G2/M检验点的天然产物抑制剂的全合成与化学生物学研究
立项时间: 2011-2013 项目经费：350000

5. 小分子探针导向的化学生物学
立项时间: 2017-2021 项目经费：3500000

6. 从传统中药中提取的抗癌天然产物的全合成研究
立项时间: 2009-2011 项目经费：180000

7. 靶向肝纤维化的化学遗传学研究
立项时间: 2023

8. 三尖杉碱生物合成研究中酶反应标准产物的化学合成
立项时间: 2020-2020

9. 源于泰国传统药用植物的、具有抗糖尿病活性天然产物的发现，合成与化学生物学研究
立项时间: 2020-2022

10. 抗骨髓瘤药物靶点DYRK2激酶动态修饰蛋白酶体的特异性化学干预
立项时间: 2019-2022

技术咨询