(1) 基于靶点的小分子药物设计
(2) 活性天然产物的结构改造与修饰
(3) 新型小分子降解剂开发

(1) 国家自然科学基金委员会, 面上项目, 82574253, 下调线粒体转录的新型POLRMT抑制剂及降解剂的设计、合成与抗肿瘤活性评价, 2026-01-01 至 2029-12-31, 49万元, 在研, 主持
(1) 江苏省科技厅, 江苏省自然科学基金面上项目, BK20231483, 新型 POLRMT 抑制剂的设计、合成与抗肿瘤活性评价, 2023-08-01 至 2026-7-31, 10万元, 在研, 主持
(3) 国家自然科学基金委员会, 青年科学基金项目, 81903446, 新型NLRP3非ATP竞争性抑制剂的设计及其抗肺癌活性探索研究, 2020-01-01 至 2022-12-31, 21万元, 结题, 主持
(4) 教育部, 中央高校基本科研业务费重点项目, 2632022ZD14, 具有新结合模式的新型NLRP3小分子抑制剂的探索研究, 2021-12 至 2023-12, 20万元, 结题, 主持
(5) 中国博士后科学基金会, 中国博士后科学基金面上资助, 2019M652037, 以冬凌草甲素为模板的新型NLRP3抑制剂探索研究, 2019-12 至 2022-06, 8万元, 结题, 主持
(6) 江苏省科技厅, 江苏省自然科学基金青年基金项目, BK20190564, 基于冬凌草甲素设计新型 NLRP3非ATP竞争性抑制剂, 2019-07 至 2022-06, 20万元, 在研, 主持
(7) 江苏省人力资源和社会保障厅, 江苏省博士后科学基金, 2019Z379, 江苏省博士后日常资助, 2019-12 至 2021-11, 16万元, 结题, 主持
(8) 国家自然科学基金委员会, 面上项目, 82073809, 手性功能化纳米材料毛细管电色谱拆分新系统及其机理研究, 2021-01-01 至 2024-12-31, 55万元, 在研, 参与
(9) 国家自然科学基金委员会, 面上项目, 81973167, 基于秋水仙碱结合位点的新型多功能肿瘤血管破坏 剂的研究, 2020-01-01 至 2023-12-31, 55万元, 在研, 参与
(10) 国家自然科学基金委员会, 面上项目, 81874289, 基于天然活性产物XJP的新型多靶点抗AD药物分子发 现研究, 2019-01-01 至 2022-12-31, 57万元, 在研, 参与

1.Dazhi Feng#, Xinnan Li#, Junkai Liu#, Xiao Shao, Lihua Liu, Yuning Shi, Yunyue Wang, Minghui Yu, Shuangtian Tang, Li Deng, Yongjie Zhang, Shaowen Xie, Jinyi Xu*, Shengtao Xu*, Hong Yao*.Selectively triggered: ROS-activated Michael acceptor prodrug strategy to enhance tumor targeting efficacy. Chem. Sci., 2025, 16, 15628-15637.
2.Xinnan Li#, Lihua Liu#, Dazhi Feng#, Yuning Shi, Lijuan Huang, Minghui Yu, Xiawei Fu, Li Deng, Xinyang Nie, Cong Chen, Yifan Yuan, Moyang Guo, Chen Chen, Yongjie Zhang*, Fangrong Zhang*, Hong Yao*. Design, Optimization, and Biological Evaluation of a Novel Quinoline-Based POLRMT Inhibitor for Prostate Cancer Therapy. J. Med. Chem. 2025, 68, 15, 15495–15519.
3.Shaowen Xie#, Jingjie Zhu#, Fangyi Zhan, Dazhi Feng, Chen He, Lihua Liu, Jia Xie, Jingyu Liu, Ming Zhong, Xingting Zhang, Jinyi Xu,* Hong Yao,* Shengtao Xu*.Overcoming E3 Ligase-Mediated Resistance: Development of Novel Hydrophobic Tagging-Based Degraders Targeting ALK Protein. J. Med. Chem. 2025, 68, 15, 15579–15597.
4.Shengnan Zhou#, Xiaotong Ze#, Dazhi Feng#, Lihua Liu, Yuning Shi, Minghui Yu, Lijuan Huang, Yunyue Wang, Hanlu Men, Jianbing Wu, Zhenwei Yuan, Mengze Zhou, Jinyi Xu*, Xinnan Li*, Hong Yao*. Identification of 6-Fluorine-Substituted Coumarin Analogues as POLRMT Inhibitors with High Potency and Safety for Treatment of Pancreatic Cancer. J. Med. Chem. 2024, 67, 13231–13251
5.Chen He#, Junkai Liu#, Junda Li#, Hongyu Wu, Chenyang Jiao, Xiaotong Ze, Shengtao Xu*, Zheying Zhu, Wenjie Guo*, Jinyi Xu*, Hong Yao*. Hit-to-Lead Optimization of the Natural Product Oridonin as Novel NLRP3 Inflammasome Inhibitors with Potent Anti-Inflammation Activity. J. Med. Chem. 2024, 67, 9406–9430.
6.Xinnan Li#, Xiaotong Ze, Shengnan Zhou, Zhaoxin Hu, Chen He, Yilin Jia, Lihua Liu, Tao Wang, Junda Li, Shengtao Xu, Dong-Hua Yang, Zhe-sheng Chen, Hequan Yao*, Jinyi Xu*, Hong Yao*. Discovery of a Novel, Potent, Orally Active, and Safe Inhibitor Targeting Human Mitochondrial RNA Polymerase. J. Med. Chem. 2023, 66, 5118–5153.
7.Shaowen Xie#, Feiyan Zhan, Jingjie Zhu, Yuan Sun, Huajian Zhu, Jie Liu, Jian Chen, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Hong Yao*, Jinyi Xu*, Shengtao Xu*. Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation. Angew. Chem. Int. Ed. 2023, 62, e2022172461.
8.Shaowen Xie,# Jingjie Zhu,# Junda Li, Feiyan Zhan, Hong Yao,* Jinyi Xu,* Shengtao Xu*. Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation. J. Med. Chem. 2023, 66, 10917–10933.
9.Hongyu Wu#, Hong Yao#,*, Chen He, Yilin Jia, Zheying Zhu, Shengtao Xu*, Dahong Li, Jinyi Xu*. Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment. Acta Pharm. Sin. B 2022, 12, 3548-3566.
10.Hong Yao#, Giuseppe Uras#, Pengfei Zhang#, Shengtao Xu, Ying Yin, Jie Liu, Shuai Qin, Xinuo Li, Stephanie  Allen, Renren Bai, Qi Gong, Haiyan Zhang*, Zheying Zhu*, and Jinyi Xu*. Discovery of Novel Tacrine−Pyrimidone Hybrids as Potent Dual AChE/GSK3 Inhibitors for the Treatment of Alzheimer’s Disease. J. Med. Chem. 2021, 64, 7483−7506.

博士研究生
冯大智（2023级）
陈聪（2024级）
刘丽华（2025级）
硕士研究生
史宇宁（2023级）
黄丽娟（2024级）
于明卉（2024级）
汪云跃（2024级）
聂新阳（2024级）
唐双甜（2025级）
袁逸凡（2025级）
周洁雅（2025级）