陆晓杰

男， 中国科学院上海药物研究所， 教授/研究员/教授级高工或同等级别

学习/工作经历

2017.7-至今
上海药物研究所，课题组长，研究员
   
2016.5-2017.6
葛兰素史克, 美国波士顿， Associate Fellow
   
2010.11-2016.5
葛兰素史克, 美国波士顿, 研究员

2007.9-2011.5 Brandeis University, 有机化学博士

2005.9-2007.8 Brandeis University, 有机化学硕士

2001.9-2005.6 南京大学，化学本科

研究领域和兴趣

化学生物学和药物发现

主要业绩

陆晓杰课题组长期致力于核酸编码化合库（DEL）技术的开发和应用研究，通过将DEL技术和其他药物开发技术（人工智能药物设计、化学蛋白组学和天然产物药物开发等）相结合，设计并合成针对特定靶点的DEL库来加快小分子、环肽和核酸等药物的开发。课题组开发了一系列可用于DEL构建的化学反应工具，扩展了和核酸相容的化学反应类型，丰富了DEL的化学空间；建立了完整的DEL设计、合成、筛选和数据分析验证的技术平台，为新靶点活性小分子苗头化合物的发现提供了有力的技术支持。先后承担了国家自然科学基金重点、面上项目等多个项目。近五年在J. Am. Chem. Soc.、Angew. Chem. Int. Ed.、Chem. Sci.、J. Med. Chem.等期刊发表SCI文章40余篇。

 

代表成果

1. Xinyuan Wu, Jiayi Pan, Rufeng Fan, Yiwei Zhang, Chao Wang, Guoliang Wang, Jiaxiang Liu, Mengqing Cui, Jinfeng Yue, Rui Jin, Zhiqiang Duan, Mingyue Zheng, Lianghe Mei, Lu Zhou, Minjia Tan*, Jing Ai*, Xiaojie Lu*；Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads，J. Am. Chem. Soc. 2025，DOI: 10.1021/jacs.5c01712

2. 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, Xiao-Hua Chen, Yujun Zhao, Mingyue Zheng, Yi Sun*, Lu Zhou*, Xiaojie Lu*; Proteome-Wide Data Guides the Discovery of Lysine-Targeting Covalent Inhibitors Using DNA-Encoded Chemical Libraries, Angew. Chem. Int. Ed., 2025，https://doi.org/10.1002/anie.202505581

3. Yuhan Gui, Rui Hou, Yuchen Huang, Yu Zhou, Shihao Liu, Ling Meng, Ying Li, Fong Sang Lam, Ruoyun Ding, Yan Cao, Gang Li*, Xiaojie Lu*, Xiaoyu Li*；Discovering Cell‐Targeting Ligands and Cell‐Surface Receptors by Selection of DNA‐Encoded Chemical Libraries against Cancer Cells without Predefined Targets；Angew. Chem. Int. Ed., 2025, https://doi.org/10.1002/ange.202421172

4. Xudong Wang, Liwei Xiong, Ying Zhu, Sixiu Liu, Wenfeng Zhao, Xinyuan Wu, Mengnisa Seydimemet, Linjie Li, Peiqi Ding, Xian Lin, Jiaxiang Liu, Xuan Wang, Zhiqiang Duan, Weiwei Lu, Yanrui Suo, Mengqing Cui, Jinfeng Yue, Rui Jin, Mingyue Zheng, Yechun Xu, Lianghe Mei*, Hangchen Hu*, and Xiaojie Lu*；Covalent DNA-Encoded Library Workflow Drives Discovery of SARS-CoV-2 Nonstructural Protein Inhibitors； J. Am. Chem. Soc. 2024，146, 33983-33996.

5. Yanrui Suo,‡ Xu Qian,‡ Zhaoping Xiong, Xiaohong Liu, Chao Wang, Baiyang Mu, Xinyuan Wu,Weiwei Lu, Meiying Cui, Jiaxiang Liu, Yujie Chen, Mingyue Zheng*, and Xiaojie Lu*; Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy; J. Med. Chem. 2024, 67, 18969-18980.

6. Qin S, Feng L, Zhao Q, Yan Z, Lyu X, Li K, Mu B, Chen Y, Lu W, Wang C, Suo Y, Yue J, Cui M, Li Y, Zhao Y*, Duan Z*, Zhu J*, Lu X*. Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach. J Med Chem. 2024 67, 1079-1092.

7. Lulu Jiang, Sixiu Liu, Xinglong Jia, Qinting Gong, Xin Wen, Weiwei Lu, Jintong Yang, Xinyuan Wu, Xuan Wang, Yanrui Suo, Yilin Li, Motonari Uesugi, Zhi-bei Qu, Minjia Tan*, Xiaojie Lu* and Lu Zhou*，ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery of Tyrosine-Targeting Covalent Inhibitors from DNA-Encoded Libraries，J. Am. Chem. Soc. 2023, 46, 25283–25292

8. Wen X, Zhang M, Duan Z, Suo Y, Lu W, Jin R, Mu B, Li K, Zhang X, Meng L, Hong Y, Wang X, Hu H, Zhu J, Song W, Shen A*, Lu X*. Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library. J Med Chem. 2023，66, 11118–11132 

9. Yang P, Wang X, Li B, Yang Y, Yue J, Suo Y, Tong H, He G, Lu X*, Chen G*. Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA. Chem Sci. 2021, 12, 5804-5810.

10. Wang X, Liu J, Yan Z, Liu X, Liu S, Suo Y, Lu W, Yue J, Chen K, Jiang H, Zhao Y*, Zheng M*, Dai D*, Lu X*. Diversified strategy for the synthesis of DNA-encoded oxindole libraries. Chem Sci. 2021, 12, 2841-2847. 

*以上信息由高级会员个人更新和维护。