ZHAO, Yujun

Academic Appointments

12/2025- College of Pharmaceutical Science, Zhejiang University of Technology

Professor

09/2025-11/2025 School of Pharmaceutical Sciences (Shenzhen), Sun Yat-Sen University

Professor 

03/2015-08/2025 Division of Medicinal Chemistry, Shanghai Institute of Materia Medica

Chinese Academy of Science

Professor and Principle Investigator

04/2012–03/2015 Division of Hematology/Oncology, Department of Internal Medicine

University of Michigan, Ann Arbor, Michigan, USA

Research Investigator  

06/2009–03/2012 Division of Hematology/Oncology, Department of Internal Medicine 

University of Michigan, Ann Arbor, Michigan, USA

Postdoctoral Research Fellow

06/2008–05/2009 Division of Chemistry and Biological Chemistry

School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore

Project Officer

Education 

05/2005-11/2008  Nanyang Technological University, Singapore

Ph.D in organic chemistry

08/2003-04/2005  National University of Singapore, Singapore

09/1999-06/2003  Soochow University, Jiangsu Province, P. R. China

Bachelor in Chemistry Education

Contribution to textbooks:

1. Advanced Medicinal Chemistry: Strategies for Drug Discovery and Structural Optimization, edited by Liu Hong and Chen Kaixian, Science Press, 2025, ISBN 978-7-03-082182-9, Chapter 24: Optimization Strategies for Enhancing the Blood-Brain Barrier Permeability of Lead Compounds

(a) 2021, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Most Popular Teaching Award

1. National Natural Science Foundation of China, General Program, 82574229, Synthesis of BFL-1 Inhibitors and PROTAC Degraders to Investigate Their Pharmacological Activity in Overcoming Venetoclax Resistance, 2026-01 to 2029-12, 490,000 RMB, Principal Investigator.

2. National Natural Science Foundation of China, General Program, 82273759, Design and Synthesis of Dual-Target MDM2/4 Small Molecule Inhibitors and PROTAC Degraders, and Investigation of Their Biological Activity, 2023-01 to 2026-12, 520,000 RMB, Principal Investigator.

3. Research on Clinical Candidate Molecules of Dual-Target MDM2/4 Small Molecule Inhibitors and PROTAC Degraders, Shanghai Institute of Materia Medica, Chinese Academy of Sciences Independent Research Project, SIMM0320231008, 2023/10-2025/09, 2,000,000 RMB, Principal Investigator.

4. Shanghai Natural Science Foundation, General Program, 22ZR1474500, Design and Synthesis of Dual-Target MDM2/4 Inhibitors and Investigation of Their Anti-Tumor Activity, 2022-04 to 2025-03, 200,000 RMB, Principal Investigator.

5. National Natural Science Foundation of China, General Program, 82073682, Development of TEAD-YAP Protein-Protein Interaction Small Molecule Inhibitors and Investigation of Their Activity, 2021-01 to 2024-12, 560,000 RMB, Principal Investigator.

6. National Natural Science Foundation of China, General Program, 81872724, Design and Synthesis of Novel MAP3K14 Kinase Inhibitors and Degraders, and Investigation of Their Biological Activity and Druggability, 2019-01 to 2022-12, 570,000 RMB, Principal Investigator.

7. National Natural Science Foundation of China, General Program, 81673295, Design and Synthesis of BET-Bromodomain Small Molecule Inhibitors and BET Protein Degraders, and Investigation of Their Epigenetic Properties, 2017-01 to 2020-12, 590,000 RMB, Principal Investigator.

8. National Science and Technology Major Project for Significant New Drugs Development, Sub-project Title: Key Technologies for New Drug Research Based on Regulation of Post-Translational Modifications, 2018ZX09711002-004-010, Development of Novel NIK Inhibitors to Regulate IKKα Phosphorylation and p100 Degradation, and Investigation of Their Druggability, 2018-01 to 2020-12, 1,157,300 RMB, Principal Investigator.

9. Chinese Academy of Sciences Strategic Priority Research Program (Category A), Project Four, Sub-project 29, XDA12040329, Design, Synthesis and Activity Study of Novel ASK1 Kinase Inhibitors, 2019-01 to 2020-09, 860,500 RMB,  Principal Investigator.

10. Chinese Academy of Sciences Strategic Priority Research Program (Category A), Project Two, Sub-project 22, XDA12020322, Development of Epigenetic BET Bromodomain Small Molecule Inhibitors and Investigation of Their Drug Resistance, 2016-01 to 2017-12, 1,000,000 RMB, Principal Investigator.

11. Jinan Natural Science Foundation, Introduced Innovation Team Project, 2021GXRC069, Innovation Team for Research and Development of Tumor-Targeting New Drugs Targeting Protein-Protein Interactions, 2022-01 to 2024-12, 1,200,000 RMB, Principal Investigator.

Peer-reviewed Publications:

1. Shijie Zhang, Xi Zhang, Jianfeng Lou, Hongyan Jing, Ziqin Yan, Yi Wang, Yuting Gui, Lan Xu, Xilin Lyu, Yuhang Lu, Zhiyi Wang, Chen Liu, Xiao Xiao, Linghua Meng*, Yujun Zhao*, N-Iminopyridinium ylides as chemically stable pharmacophores enabling targeted degradation of SMARCA proteins, JACS Au, 2026, 6, DOI:  10.1021/jacsau.6c00022, (IF: 8.7, Year 2025) (15/15)     

2. Xilin Lyu, Xiancheng Wang, Dongze Lin, Yuhan Lu, Chenxu Wang, Ziqin Yan, Zhiyi Wang, Ying Cheng, Jing Cheng, Xuelian Ren, Yi Su, Shijie Zhang, Yi Chen,* He Huang,* Yujun Zhao* Synthesis of an RBM39 degrader that downregulates CEP192 and induces disorganized spindle structures, Journal of Medicinal Chemistry, 2025, 68, 7807–7826 (IF: 6.8, Year 2024)    

3. Yuhang Lu, Ziqin Yan, Jiaqi Sun, Chenxu Wang, Lan Xu, Xilin Lyu, Xiancheng Wang, Jianfeng Lou, He Huang,* Linghua Meng,* Yujun Zhao*, Selective degradation of TEADs by a PROTAC molecule exhibited robust anticancer efficacy in vitro and in vivo, Journal of Medicinal Chemistry, 2025, 68, 5616-5640. (IF: 6.8, Year 2024)  

4. Hanqing Zhao, Xue Li, Xueyu Yao, Shijie Zhang, Yandan Bao, Weiwei Lu, Minyan Xing, Xudong Wang, Xuan Wang,* Yujun Zhao,* Qian Chu,* and Xiaojie Lu*, Influence of macrocyclization strategies on DNA-encoded cyclic 2 peptide libraries, JACS Au, 2025, 5, 3399−3407. (IF: 8.7, Year 2025)  

5. Zhiyi Wang, Shijie Zhang, Loïca Mélita Irakoze, Yujun Zhao* Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema, European Journal of Medicinal Chemistry, 2025, 117909. (IF: 5.9, Year 2024)  

6. Huan Ling, Lin Li, Liping Duan, Weixue Huang, Jiangnan Zheng, Shijie Zhang, Xinling Li, Xiaorong Qiu, Yang Zhou, Nan Ma, Xiaomei Ren, Jinwei Zhang, Zhen Wang, Yujun Zhao, Ruijun Tian, Zhi-Min Zhang*, and Ke Ding,* O-Cyanobenzaldehydes irreversibly modify both buried and exposed lysine residues in live cells, Journal of American Chemical Society, 2025, 147, 14, 11955–11963 (IF: 14.5, Year 2024)

7. Xinyuan Wu, Shunyao Li, Ting Liang, Qing Yu, Yiwei Zhang, Jiaxiang Liu, Kaige Li, Zijian Liu, Mengqing Cui, Yongchao Zhao, Xin Han, Rui Jin, Minjia Tan, Xiaohua Chen, Yujun Zhao, Mingyue Zheng, Yi Sun,* Lu Zhou,* and Xiaojie Lu,* Proteome-wide data guides the discovery of lysine-targeting covalent inhibitors using DNA-encoded chemical libraries, Angewandte Chemie International Edition, 2025, 64(25):e202505581. (IF: 16.6, Year 2024)

8. MDM2-p53相互作用抑制剂的研究进展和临床现状，张世界，赵玉军，《药学进展》，2025，49卷，8期，612页。 

9. Jianfeng Lou, Qianqian Zhou, Xilin Lyu, Xinyi Cen, Chen Liu, Ziqin Yan, Yan Li, Haotian Tang, Qiupei Liu, Jian Ding, Ye Lu, He Huang,* Hua Xie,* Yujun Zhao,* Discovery of a covalent inhibitor that overcame resistance to Venetoclax in AML cells overexpressing BFL-1, Journal of Medicinal Chemistry, 2024, 67, 10795-10830. (IF: 6.8, Year 2024)  

10. Zhitong Lin, Chen Liu, Ziqin Yan, Jing Cheng,Xiancheng Wang, Feilong Zhou, Xilin Lyu, Shiyan Zhang, Daizhou Zhang, Xiangjing Meng,*Yujun Zhao*, Synthesis and Biological Evaluation of 4-Imidazolidinone–Containing Compounds as Potent Inhibitors of the MDM2/p53 Interaction, European Journal of Medicinal Chemistry, 2024, 116366. (IF: 6.0, Year 2024)    

11. Shaozhao Qin, Lijian Feng, Qingyi Zhao, Ziqin Yan, Xilin Lyu, Kaige Li, Baiyang Mu, Yujie Chen, Weiwei Lu, Chao Wang, Yanrui Suo, Jinfeng Yue, Mengqing Cui, Yingjie Li, Yujun Zhao,* Zhiqiang Duan,* Jidong Zhu,* and Xiaojie Lu,* Discovery and Optimization of WDR5 Inhibitors via Cascade 2 Deoxyribonucleic Acid-Encoded Library Selection Approach, Journal of Medicinal Chemistry, 2024, 67, 1079-1092. (IF: 6.8, Year 2024)  

12. Wenhua Zhu, Cuiting Liu, Kang Xi, Anqi Li, Lian Shen, Yana Li, Miaomiao Jia, Yangbo He, Gang Chen, Chenglong Liu, Yangqiang Chen, Kai Chen, Fan Sun, Daizhou Zhang, Chonggang Duan, Heng Wang, Dongdong Wang, Yujun Zhao,* Xiangjing Meng,* Di Zhu,* Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy Through the Activation of Antigen Presentation of cDC1 Cells, Journal of Medicinal Chemistry, 2024, 67, 12485-12520. (IF: 6.8, Year 2024)  

13. Jing Cheng, Ziqin Yan, Xinzhi Li, Chen Liu, Linjiang Tong, Xilin Lyu, Bingjie Yang, Zheng Chen,* Yujun Zhao*, Structure-based optimization of indoline-containing compounds as second generation inhibitors of NF-κB-inducing kinase (NIK). Journal of Molecular Structure, 2024, 136755. (IF: 4.0, Year 2024)   

14. Bo Hou, Jiayi Ye, Lujia Huang, Wenhao Cheng, Fangmin Chen, Huiling Zhou, Jiaxing Pan, Jing Gao, Yi Lai, Yujun Zhao, Wei Huang, Haijun Yu, Zhiai Xu* Tumor-specific delivery of clickable inhibitor for PD-L1 degradation and mitigating resistance of radioimmunotherapy, Science Advances, 2024, 10, eadq3940  (IF: 11.7, Year 2024)

15. Jing Cheng, Ziqin Yan, Kailong Jiang, Chen Liu, Dehua Xu, Xilin Lyu, Xiaobei Hu, Shiyan Zhang, Yubo Zhou,* Jia Li,* Yujun Zhao*, Discovery of JN122, a Spiroindoline-containing Molecule, that Inhibits MDM2/p53 Protein-protein Interaction and Exerts Robust in vivo Antitumor Efficacy. Journal of Medicinal Chemistry, 2023, 66, 16991-17025. (IF: 7.3, Year 2023)  

16. Ziqin Yan, Xilin Lyu, Dongze Lin, Gaoxing Wu, Yang Gong, Xuelian Ren, Jian Xiao, Jianfeng Lou, He Huang, Yi Chen*, Yujun Zhao*, Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines, European Journal of Medicinal Chemistry, 2023, 115381. (IF: 6.7, Year 2023)  

17. Ying Cheng, Xilin Lyu, Chen Liu, Xiancheng Wang, Jing Cheng, Daizhou Zhang,  Xiangjing Meng,* Yujun Zhao*, Synthesis and biological evaluation of sclareolide-indole conjugates and their derivatives. Molecules, 2023, 28, 1737. (IF: 4.92, Year 2022)  

18. Mengnisa Seydimemet, Yixuan Yang, Yuhan Lv, Jiaxiang Liu, Ziqin Yan, Yujun Zhao*, Xuan Wang*, Xiaojie Lu*, Design, construction, and screening of diversified pyrimidine-focused DNA-encoded libraries, ACS Med. Chem. Lett. 2023, 14, 1073−1078. (IF: 4.2, Year 2022)  

19. Shiyan Zhang, Ziqin Yan, Yafang Li, Yang Gong, Xilin Lyu, Jianfeng Lou, Daizhou Zhang, Xiangjing Meng*, Yujun Zhao*, Structure-based discovery of MDM2/4 dual inhibitors that exert antitumor activities against MDM4 -overexpressing cancer cells, Journal of Medicinal Chemistry, 2022, 65, 6207-6230. (IF: 8.03, Year 2022)  

20. Xuexin Feng, Ziqin Yan, Feilong Zhou, Jianfeng Lou, Xilin Lyu, Xuelian Ren, Ziyu Zeng, Chenglong Liu, Shiyan Zhang, Di Zhu, He Huang, Jinming Yang*, Yujun Zhao*, Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells, European Journal of Medicinal Chemistry, 2022, 114327. (IF: 7.08, Year 2022)  

21. Jianfeng Lou, Yuhang Lu, Jing Cheng, Feilong Zhou, Ziqin Yan, Daizhou Zhang,Xiangjing Meng,* Yujun Zhao*, A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities, European Journal of Medicinal Chemistry, 2022, 114684. (IF: 7.08, Year 2022)  

22. Shiyan Zhang, Jianfeng Lou, Yafang Li, Feilong Zhou, Ziqin Yan, Xilin Lyu, Yujun Zhao*, Recent progress and clinical development of inhibitors that block MDM4/p53 protein-protein interactions, Journal of Medicinal Chemistry, 2021, 64, 10621–10640. (IF: 7.44, Year 2021)  

23. Chenglong Liu, Feilong Zhou, Ziqin Yan, Lian Shen, Xichen Zhang, Fenglian He, Xiaojie Lu, Heng Wang, Ker Yu, Yujun Zhao*, Di Zhu*, Discovery of a novel, potent, and selective small-molecule inhibitor of PD-1/PD-L1 interaction with robust in vivo anti-tumor efficacy, British Journal of Pharmacology, 2021, 178, 2651-2670. (IF: 8.73, Year 2021)  

24. Xuan Wang, Jiaxiang Liu, Ziqin Yan, Xiaohong Liu, Sixiu Liu, Yanrui Suo, Weiwei Lu, Jinfeng Yue, Kaixian Chen, Hualiang Jiang, Yujun Zhao*, Mingyue Zheng*, Dongcheng Dai*, Xiaojie Lu*, Diversified strategy for the synthesis of DNA-encoded oxindole libraries, Chemical Science, 2021, 12, 2841-2847. (IF: 9.82, Year 2021)  

25. Jing Cheng, Xuexin Feng, Zhiqiang Li, Feilong Zhou, Jin-Ming Yang, Yujun Zhao*, Pharmacological inhibition of NF-κB-inducing Kinase (NIK) with small molecules for the treatment of human diseases, RSC Medicinal Chemistry, 2021, 12, 552-565.  

26. Xian Zhou, Xuexin Feng, Dachi Wang, Deheng Chen, Gaoxing Wu, Ziqin Yan, Xilin Lyu, Huan Wang, Jin-Ming Yang,* Yujun Zhao*, Synthesis and bioactivity studies of covalent inhibitors derived from (-)-Chaetominine, Journal of Molecular Structure, 2021, 1241, 130694. (IF: 3.19, Year 2021)  

27. Xinzhi Li, Bingchuan Yuan, Min Lu , Yuqin Wang, Na Ding, Chunhong Liu, Ming Gao, Zhicheng Yao, Shiyan Zhang, Yujun Zhao, Liwei Xie, Zheng Chen*,The methyltransferase METTL3 negatively regulates nonalcoholic steatohepatitis (NASH) progression, Nature Communications, 2021, 12, 7213.

28. Zhiqiang Li, Xinzhi Li, Ming-Bo Su, Li-Xin Gao, Yu-Bo Zhou, Bingchuan Yuan, Xilin Lyu, Ziqin Yan, Chujiao Hu, Hao Zhang, Cheng Luo, Zheng Chen*, Jia Li*, Yujun Zhao*, Discovery of a potent and selective NF-κB-inducing kinase (NIK) inhibitor that has anti-inflammatory effects in vitro and in vivo, Journal of Medicinal Chemistry, 2020, 63, 4388-4407. (IF: 7.44, Year 2021)  

29. Shiyan Zhang, Chaoying Huang, Xilin Lyu, Peipei Wang, Yi Zang, Zengtao Wang, Huan Wang, Jia Li*, Yujun Zhao*, Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal -regulating kinase 1 (ASK1), European Journal of Medicinal Chemistry, 2020, 195, 112277. (IF: 6.51, Year 2021)  

30. Xinzhi Li, Yongsen Wu, Yue Song, Na Ding, Min Lu, Linna Jia, Yujun Zhao, Ming Liu, Zheng Chen*, Activation of NF-kB-inducing kinase in islet β-cells causes β-cell failure and diabetes, Molecular Therapy, 2020, 2430-2441. (IF: 11.45, Year 2021)

31. Deheng Chen, Tian Lu, Ziqin Yan, Wenchao Lu, Feilong Zhou, Xilin Lyu, Biling Xu, Hualiang Jiang, Kaixian Chen, Cheng Luo*, and Yujun Zhao*, Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins, European Journal of Medicinal Chemistry, 2019, 182, 111633. (IF: 6.51, Year 2021)  

32. Erbao Zhao, Feilong Zhou, and Yujun Zhao*, Lewis Acids Promoted 3+2 Cycloaddition of Oxaziridines and Cyclic Allylic Alcohols through Carbonyl Imine Intermediates, Journal of Organic Chemistry, 2019, 84 (7), 4282–4293. (IF: 4.35, Year 2021)     

33. Deheng Chen, Dexiang Guo, Ziqin Yan, Yujun Zhao*, Allenamide as a bioisostere of acrylamide in design and synthesis of targeted covalent inhibitors Med. Chem. Commun. 2018, 9, 244-253. (IF: 2.80, Year 2020)    

34. Feilong Zhou, Erbao Zhao, Ziqin Yan, Deheng Chen, Yujun Zhao*, Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles, Tetrahedron Letters, 2018, 59, 1871-1874. (IF: 2.41, Year 2021)  

35. Xiaomeng Ren, Xinzhi Li, Linna Jia, Deheng Chen, Hai Hou, Liangyou Rui, Yujun Zhao*, Zheng Chen*, A small-molecule inhibitor of NF-kB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury, FASEB Journal. 2017, 2, 711-718. (IF: 5.19, Year 2021)  

Book Chapters:

1. Yujun Zhao, Luhang Lu, Ziqin Yan, Xilin Lyu, Shijie Zhang, Chapter 16. Belzutifan: a first-in-class oral HIF-2α inhibitor approved for patients with Von Hippel-Landau (VHL) disease-associated renal cell carcinoma, Book: Drug Discovery Stories, Volume 2, Editors Bin Yu and Peng Zhan, ISBN: 9780443338854, eBook ISBN: 9780443338861, Elsevier, October 1, 2025.

2. Yujun Zhao, Jianfeng Lou, Yuhang Lu, Feilong Zhou, Ziqin Yan, Chapter 4: The N-sulfonyl carboxamide moiety as a privileged structure in approved drugs, Book: Privileged Scaffolds in Drug Discovery, Academic Press, ISBN: 9780443186110, 2023, 65-80.

3. Shaomeng Wang, Yujun Zhao, Denzil Bernard, Angelo Aguilar, Sanjeev Kumar, Chapter: Protein-Protein Interactions, Book: Targeting the MDM2-p53 Protein-Protein Interaction for New Cancer Therapeutics, Springer-Verlag Berlin Heidelber, 2012, Vol. 8, 57-80. 

1. Guest Editor and Section Board Member of Molecules

2. Guest Editor and Editorial Board Member of Scientific Reports 

3. 全国卫生产业企业管理协会精准医疗分会, 常务理事 (2024-2029)