YANG Weibo
Principal Investigator
Small-Molecule Drug Research Center
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CONTACT
yweibo@simm.ac.cn
021-68077996
201203
555 Zu Chong Zhi Road, Pudong, Shanghai, P.R.China
Biography
YANG Weibo, Ph.D., Principal investigator of Shanghai Institute of Materia Medica, Chinese Academy of Sciences. Dr. Yang received MSc from Dalian University of Science and Technology in 2010 and his Ph.D in chemistry from University of Heidelberg in 2013. After he obtained his PhD under the supervision of Prof. Stephen Hashmi in 2013, he joined the laboratory of Prof. Jin-Quan Yu at the Scripps Research Institute as a research associate. In 2015, he joined Prof. Peter G Schultz as a research associate. Since Oct. 2016, Dr. Yang has worked at Shanghai Institute of Materia Medica, Chinese Academy of Sciences. His current research interest is mainly focused on the studying on the transition-metal-catalyzed rearrangement, domino as well as C–H activation reactions and their applications in medicinal chemistry. EDUCATION 2015.12–2016.10: Associate Researcher, The Scripps Research Institute, CA, USA; with Prof. Peter G Schultz; Medicinal Chemistry. 2013.12–2015.12: Associate Researcher, The Scripps Research Institute, CA, USA; with Prof. Dr. Jin-quan Yu; Organic Chemistry. 2013.9–2013.11: Research Assistant, Heidelberg University, Germany; with Prof. Dr. Stephen Hashmi; Organic Chemistry. 2010.9–2013.8: Ph. D., Heidelberg University, Germany; guided by Prof. Dr. Stephen Hashmi; Organic Chemistry. 2007.9–2010.7: M. S., Dalian University of Technology, Dalian, China; guided by Prof. Chun Liu; Applied Chemistry. WORK EXPERIENCE Oct 2016–Present Professor , Principal Investigator Small-Molecule Drug Research Center,Shanghai Institute of Materia Medica, CAS.
Research Directions
Metal catalysis, C-H activation, mechanistic research on organic reactions, Natural product-inspired Macrocyclic compounds synthesis, Protein-Protein interaction inhibitors design
Grants & Research Projects
1. 2018.1 -2020.12, National Natural Science Foundationof China (21702217)
2. 2022.1- 2025.12, National Natural Science Foundationof China (22171275)
3. 2024.1-2027.12, National Natural Science Foundationof China (82373708)
4. 2023.5.1-2026.4.3, Program of Shanghai Academic/Technology Research Leader(Number: 23XD1424400)
5. 2018.1.1-2020.12.31, National Science &Technology Major Project “Key New Drug Creation andManufacturing Program” China (Number:2018ZX09711002-006)
6. 2018.12.1-2021.11.30, Science and Technology Commissionof Shanghai Municipality (18431907100)
7. 2018.6.1- 2021.5.31, Shanghai-TechnologyInnovation Action Plan (18JC1415300)
8. 2019.4.1- 2022.3.31, Shanghai“Phosphor” Science Foundation (19QA1410700)
9. 2024.1.1-2026.12.31, Shanghai Leading TalentProgram2022
Achievements
1) Developed highly efficient and low-toxicity macrocyclic lactam inhibitors for tumor multidrug resistance and revealed a novel mechanism of action involving protein interaction regulation and conformation changes;
2) Discovered highly selective macrocyclic oxime inhibitors against the H1N1 virus and validated their mechanism of targeting hemagglutinin to block viral invasion;
3) Elucidated the SIRT3 activation mechanism for Parkinson's disease (PD) treatment and originally developed spiro-macrocyclic SIRT3 agonists. These findings provide a novel material foundation for the development of innovative drugs targeting tumor multidrug resistance, Parkinson's disease, inflammation, and viral infections.
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Social Titles
1. Green Synthesis and Catalysis, Youth Editor
2. Chinese Journal of Natural Medicines, Youth Editor
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Awards & Honors
Liaoning outstanding graduates 2010 CSC Fellowship Evonic Degussa Award Thieme Chemistry Journal Award 2017 Shanghai-Youth Talent 2017 Shanghai“Phosphor” Talents 2019 Shanghai Leading Talent 2022 Excellent Mentor, Chinese Academy of Sciences 2022 Shanghai Academic/Technology Research Leader 2023 Pudong New Area Pearl Elite Talents 2023
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Pubilcations
Full Publication List
Selected Publications
1. Tongyu Bi,+Yunxia Cui,+Shuai Liu,+Haiyue Yu,WeirongQiu,Ke-Qiang Hou,Jiaqi Zou,Zhipeng Yu,Feili Zhang,Zhongliang Xu,Jian Zhang,* Xiaojun Xu,* Weibo Yang*, Ligand-Enabled Pd-Catalyzed sp3 C‒H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson’s Disease. Angew. Chem. Int. Ed.2024,e202412296.
2. Zhipeng Yu+, Yi Chu Liang+, Stefania Berton, Liping Liu, Jiaqi Zou, Lu Chen, Zhongliang Xu, Cheng Luo, Jim Sun*, Weibo Yang*, Small molecule targeting PPM1A activates autophagy for Mycobacterium tuberculosis host-directed therapy. J. Med. Chem.2024,67, 10, 11917– 11936.
3. Dandan Xu+, Ying Gong+, Lianju Zhang+, Fu Xiao, Xinran Wang, Ji Qin, Lin Tan, Teng Yang, Zeng Lin, Zhongliang Xu, Xiujuan Liu, Fuling Xiao, Feili Zhang, Feng Tang, JianpingZuo, Xiaomin Luo, Wei Huang*, Li Yang*, Weibo Yang*, Modular Biomimetic Strategy Enables Discovery and SAR Exploration of Oxime Macrocycles as Influenza A Virus (H1N1) Inhibitors. J. Med. Chem. 2024,67, 8201-8224.
4. Bichao Song+, Xueying Guo+, Li Yang+, Haiyue Yu, XinleiZong, Xiujuan Liu, Hao Wang, Zhongliang Xu, Zhenyang Lin*, and Weibo Yang*, Rhodium(III)-Catalyzed C-H/O2 Dual Activation and Macrocyclization: Synthesis and Evaluation of Pyrido[2,1-a]isoindole Grafted Macrocyclic Inhibitors for Influenza H1N1. Angew. Chem. Int. Ed.2023,e202218886.
5. Bo Liu+, Xueni Yu+, Liping Liu+, Lei Wang+, Jie Wang, Qianqian Huang, Zhongliang Xu, Cheng Luo, Liguang Lou*, Wei Huang*, and Weibo Yang*, Biomimetic Strategy Enabled Discovery of Simplified Pseudo-Natural Macrocyclic P‑Glycoprotein Inhibitors Capable of Overcoming Multidrug Resistance. J. Med. Chem.2023,66, 2550-2565.
6. Hao Wang+, Zhongyu Li+, Xiangyang Chen+, Jonathan J. Wong+, Tongyu Bi+, Xiankun Tong, Zhongliang Xu,Mingyue Zhen, Yunhui Wan, Li Tang, Bo Liu, XinleiZong, Dandan Xu, JianpingZuo, Li Yang*, Wei Huang*, Kendall N. Houk* and Weibo Yang*, Multicomponent coupling and macrocyclization enabled by Rh(III)-catalyzed dual C–H activation: Macrocyclic oxime inhibitor of influenza H1N1. Chem.2023, 9, 607-623(Highlighted by Science. 2022, 378, 1184-1185)
7. Stefania Berton,+ Lu Chen,+ Yi Chu Liang,+ Zhongliang Xu, Afrakoma Afriyie-Asante, NusrahRajabalee, Weibo Yang* and Jim Sun*, A selective PPM1A inhibitor activates autophagy to restrict the survival of Mycobacterium tuberculosis. Cell Chem. Biol. 2022, 29, 1126.(Highlighted by Cell Chem. Biol. 2022, 29, 1065-1067)
8. Tongyu Bi, Yi Xu, Xin Xu, Bixi Tang, Qing Yang, Yi Zang, Zhenyang Lin, Jia Li,* and Weibo Yang*, Natural scaffolds-inspired synthesis of CF3-substituted macrolides enabled by Rh-catalyzed C–H alkylation macrocyclization. Chin. Chem. Lett.2022, 33, 2015-2022.
9. Jiping Hao,+ Xueying Guo,+ Shijun He,+ Zhongliang Xu, Lu Chen, Zhongyu Li, Bichao Song JianpingZuo,Zhenyang Lin,* and Weibo Yang*, Marine furanocembranoids-inspired macrocycles enabled by Pd-catalyzed unactivated C(sp3)-H olefination mediated by donor/donor carbenes. Nat. Commun. 2021, 12, 1304.
10. Wei Shi+, Feng Tang+, JiweiAo, Qun Yu, Junjie Liu, Yubo Tang, Bofeng Jiang, Xuelian Ren, He Huang, Weibo Yang,* and Wei Huang*, Manipulating the Click Reactivity of Dibenzoazacyclooctynes: From Azide Click Component to Caged Acylation Reagent by Silver Catalysis. Angew. Chem. Int. Ed. 2020, 59, 19940-19944.
11. Bichao Song, PeipeiXie, Yingzi Li, Jiping Hao, Lu Wang, Xiangyang Chen, Zhongliang Xu, Haitian, Quan, Liguang, Lou, Yuanzhi Xia,* K. N. Houk,* and Weibo Yang*, Pd-Catalyzed Decarboxylative Olefination: Stereoselective Synthesis of PolysubstitutedButadienes and Bioactive Macrocyclic Inhibitors. J. Am. Chem. Soc. 2020, 142, 9982-9992
12. Lu Chen, Haitian Quan, Zhongliang Xu, Hao Wang, Yuanzhi Xia, Liguang Lou,* Weibo Yang,* A modular biomimetic strategy for the synthesis of macrolide P-glycoprotein inhibitors via Rh-catalyzed C-H activation. Nat. Commun. 2020, 11, 2151.
13. Yi Xu, Lu Chen, Yu-wen Yang, Zhiqiang Zhang, Weibo Yang*, Vinylethylene Carbonates as α,β-Unsaturated Aldehyde Surrogates for Regioselective [3 + 3] Cycloaddition. Org. Lett., 2019, 21, 6674-6678
14. Jiping Hao, Yi Xu, Zhongliang Xu, Zhiqiang Zhang, Weibo Yang*, Pd-Catalyzed Three-Component Domino Reaction of Vinyl Benzoxazinanones for Regioselective and Stereoselective Synthesis of Allylic Sulfone-Containing Amino Acid Derivatives. Org. Lett., 2018, 20, 7888-7892
15. Yuwen Yang, Weibo Yang*, Divergent synthesis of N-heterocycles by Pd-catalyzed controllable cyclization of vinylethylene carbonates. Chem. Commun., 2018, 24, 12182-12185
16. Lei Deng, Arjan W. Kleij,* Weibo Yang*, Diversity‐Orientated Stereoselective Synthesis through Pd‐Catalyzed Switchable Decarboxylative C-N/C-S Bond Formation in Allylic Surrogates. Chem. Eur. J., 2018, 24, 19156-19161
17. Weibo Yang, Shengqing Ye, YvonneSchmidt, Dean Stamos,*Jin-QuanYu*: Ligand-Promoted C(sp3)-H Olefination en Route to Multi-functionalized Pyrazoles. Chem. Eur. J. 2016, 22, 7059-7062.
18. Shengqing Ye, Weibo Yang, Timothy Coon, Dewey Fanning, Tim Neubert, Dean Stamos, Jin-Quan Yu*: Heterocyclic Carbene Ligand-Enabled C(sp3 )-H Arylation of Piperidine and Tetrahydropyran Derivatives. Chem. Eur. J. 2016, 22, 4748-4752.
19. Weibo Yang, Shengqing Ye, Dewey Fanning, Timothy Coon, Yvonne Schmidt, Paul Krenitsky, Dean Stamos* and Jin-Quan Yu*: Orchestrated Triple C–H Activation Reactions Using Two Directing Groups: Rapid Assembly of Complex Pyrazoles. Angew. Chem. Int. Ed. 2015, 54, 2501-2504.
20. Weibo Yang, A. Stephen K. Hashmi*: Mechanistic insights of the gold chemistry of allenes. Chem. Soc. Rev. 2014, 43, 2941–2955
21. Yang Yu+, Weibo Yang+, Daniel Pfl？sterer, A. Stephen K. Hashmi*: Dehydrogenative Meyer-Schuster-like Rearrangement: A Gold-Catalyzed Reaction Generating an Alkyne. Angew. Chem. Int. Ed. 2014, 53, 1144-1147. (Y. Yu and W. Yang contributed equally to this work)
22. Yang Yu+, Weibo Yang+, Frank Rominger, A. Stephen K. Hashmi*: In Situ Generation of Nucleophilic Allenes by the Gold-Catalyzed Rearrangement of Propargylic Esters for the Highly Diastereoselective Formation of Intermolecular C(sp3)-C(sp2) Bonds.Angew. Chem. Int. Ed. 2013, 52, 7586-7589. (Y. Yu and W. Yang contributed equally to this work)
23. A. Stephen K. Hashmi*, Weibo Yang, Yang Yu, M. Hansmann, Matthias Rudolph, Frank Rominger: Gold-Catalyzed Formal 1,6-Acyloxy Migration Leading to 3,4-Disubstituted Pyrrolidin-2-ones. Angew. Chem. Int. Ed. 2013, 52, 1329-1332. (Highlighted in Synfacts)
24. A. Stephen K. Hashmi*, Weibo Yang, Frank Rominger: Gold(I)-Catalyzed Formation of Benzo[b]furans from 3-Silyloxy-1,5-enynes. Angew. Chem. Int. Ed. 2011, 50, 5762-5765.
25. Weibo Yang, Long Huang, Yang Yu, Daniel Pflasterer, Frank Rominger, A. Stephen K. Hashmi*:HighlyDiasteroselective and Regioselective Copper-Catalyzed AcylnitrosoDearomatization Reaction under Aerobic Oxidation Conditions. Chem. Eur. J. 2014, 20, 3927-3931
26. Weibo Yang, Tao Wang, Yang Yu, Shuai Shi, Tuo Zhang, A. Stephen K. Hashmi*: Nitrones as Trapping Reagents of α,β-Unsaturated Carbene Intermediates – [1,2]Oxazino[5,4-b]indoles by a Platinum-Catalyzed Intermolecular [3+3] Cycloaddition. Adv. Synth. Catal. 2013, 355, 1523-1528. (Highlighted in Synfacts)
27. Weibo Yang, Yang Yu, Tuo Zhang, Max M. Hansmann, Daniel Pfl?sterer, A. Stephen K. Hashmi*: Gold-Catalyzed Highly Diastereoselective Synthesis of Functionalized 3,4-Disubstituted Butyrolactams via Phosphatyloxy or Carbonate Double Migrations. Adv. Synth. Catal. 2013, 355, 2037-2043. (Highlighted in Synfacts)
28. A. Stephen K. Hashmi*, Weibo Yang, Frank Rominger: Gold-Catalysis: Highly Efficient and Regio-Selective Carbonyl Migration in Alkynyl-Substituted Indole-3-Carboxamides Leading to Azepino[3,4-b]indol-1-ones. Adv, Synth, Catal. 2012, 354, 1273-1279. (Highlighted in Synfacts)
29. A. Stephen K. Hashmi*, Weibo Yang, Frank Rominger: Gold-Catalysis: Gold(I)-Catalyzed Rearrangement of 3-Silyloxy-1,5-enynes: An Efficient Synthesis of Benzo[b]thiophenes, Dibenzothiophenes, Dibenzofurans, and Indole Derivatives. Chem. Eur. J.2012, 18, 6576-6580.
22. Weibo Yang, Liu Chun*, JieshanQiu: In Situ Formation of N,O-Bidentate Ligand via the Hydrogen Bond for Highly Efficient Suzuki Reaction of Aryl Chlorides. Chem. Commun. 2010, 2659-2661. (Highlighted in Synfacts)
30. Liu Chun*, Weibo Yang: A fast and oxygen-promoted protocol for the ligand-free Suzuki reaction of 2-halogenated pyridines in aqueous media. Chem. Commun. 2009, 6267-6269.
31. A. Stephen K. Hashmi*, Tobias Haffner, Weibo Yang, Sreekumar Pankajakshan, Sascha Schafer, Lara Schultes, Frank Rominger, Wolfgang Frey: Gold Catalysis: Non-Spirocyclic Intermediates in the Conversion of Furanynes by the Formal Insertion of an Alkyne into an Aryl–Alkyl C–C Single Bond. Chem. Eur. J. 2012, 18, 10480-10486.
32. Shuai Shi, Tao Wang, Weibo Yang, Matthias Rudolph, A. Stephen K. Hashmi*: Gold Catalyzed Synthesis of Glyoxals via Oxidation of Terminal Alkynes; One-Pot Synthesis of Quinoxalines. Chem. Eur. J. 2013, 19, 6576-6580.
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