张晓进,博士,教授,博士生导师,理学院化学系主任。牛津大学(University of Oxford)访问学者。国家优秀青年基金获得者,江苏省杰青、优青基金获得者,江苏省“333高层次人才培养工程”第二层次(中青年科技领军人才)。
主持国家自然科学基金5项,企业联合攻关项目多项,担任药物分子设计校企联合实验室负责人。以通讯作者在Angewandte Chemie International Edition、Journal of Medicinal Chemistry、Chemical Science、European Journal of Medicinal Chemistry、Chemical Communications、Organic Letters等国际刊物发表论文60余篇;已授权中国、美国、欧洲、日本等国内外发明专利20余项。曾获国家科技进步奖二等奖、教育部自然科学奖一等奖、江苏省科学技术一等奖、中国药学会-施维雅青年药物化学奖。作为主要负责人之一设计研发的化药1类抗肾性贫血新药在中国进入临床试验。
研究生招生专业:药物化学(学博)、生物与医药(专博)、药物化学(学硕)、化学(学硕)、药学(专硕)
主要研究方向:围绕“细胞氧感知通路”开展靶向创新药物研发及化学生物学研究,临床需求导向的靶向药物分子设计、合成及成药性研究
实验室常用技术手段:计算机辅助药物分子设计(CADD)/ 人工智能驱动的药物设计(AIDD)/ 量子化学计算,化学合成与结构表征,靶标及细胞水平的生物活性评价,动物水平的安全性、药效学与药动学评价,临床前成药性评价等
联系方式:zxj@cpu.edu.cn 办公室:江宁校区化学楼C421
近年代表性论文:
1. Yue Wu, Yafen Chen, Thomas Corner, Yu Nakashima, Eidarus Salah, Zhihong Li, Linjian Zhang, Le Yang, Anthony Tumber, Zhuoli Sun, Yukang Wen, Ailin Zhong, Fulai Yang, Xiang Li, Zhihong Zhang, Christopher J. Schofield, Xiaojin Zhang. A small-molecule inhibitor of factor inhibiting HIF binding to a tyrosine-flip pocket for the treatment of obesity. Angewandte Chemie International Edition 2024, 63 (40), e202410438. (IF=16.1) https://doi.org/10.1002/anie.202410438
Cover: https://onlinelibrary.wiley.com/doi/10.1002/anie.202414504
2. Zhihong Li, Yue Wu, Shuai Zhen, Kaijun Su, Linjian Zhang, Fulai Yang, Michael A. McDonough, Christopher J. Schofield, Xiaojin Zhang. In situ inhibitor synthesis and screening by fluorescence polarization: an efficient approach for accelerating drug discovery. Angewandte Chemie International Edition 2022, 61 (45), e202211510. (IF=16.8) https://doi.org/10.1002/anie.202211510
3. Qijie Gong, Xiang Li, Tian Li, Xingsen Wu, Jiabao Hu, Fulai Yang, Xiaojin Zhang. A carbon-carbon bond cleavage–based prodrug activation strategy applied to β-lapachone for cancer-specific targeting. Angewandte Chemie International Edition 2022, 61 (40), e202210001. (IF=16.8) https://doi.org/10.1002/anie.202210001
4. Yue Wu, Zewei Zhang, Haiping Cai, Weiqing Zhang, Linjian Zhang, Zhihong Li, Le Yang, Yafen Chen, Thomas Corner, Zhe Song, Jie Yue, Fulai Yang, Xiang Li, Christopher J. Schofield, Xiaojin Zhang. Discovery of ZG-2305, an orally bioavailable factor inhibiting HIF inhibitor for the treatment of obesity and fatty liver disease. Journal of Medicinal Chemistry 2024 https://doi.org/10.1021/acs.jmedchem.4c01698
5. Xinye Yang, Yong Li, Shengqiang Pan, Facheng Ma, Hong Chen, Jinhui Deng, Jie Yue, Qijie Gong, Mi Zheng, Ying Zeng, Jing Li, Yingjun Zhang, Xiaojun Wang, Xiaojin Zhang. Discovery of a potent and orally bioavailable xanthine oxidase/urate transporter 1 dual inhibitor as a potential treatment for hyperuricemia and gout. Journal of Medicinal Chemistry 2024, 67 (16), 14668–14691. https://doi.org/10.1021/acs.jmedchem.4c01480
6. Yue Wu, Linjian Zhang, Zhuoli Sun, Xusheng Qiu, Yafen Chen, Kaijun Su, Le Yang, Zhongqiu Du, Ying Dong, Fulai Yang, Xiang Li, Xiaojin Zhang. Preferred conformation-guided discovery of potent and orally active HIF prolyl hydroxylase 2 inhibitors for the treatment of anemia. Journal of Medicinal Chemistry 2023, 66 (13), 8545–8563. https://doi.org/10.1021/acs.jmedchem.3c00231
7. Yancheng Yu, Fulai Yang, Quanwei Yu, Simeng Liu, Chenyang Wu, Kaijun Su, Le Yang, Xiaoqian Bao, Zhihong Li, Xiang Li, Xiaojin Zhang. Discovery of a potent and orally bioavailable hypoxia-inducible factor 2α (HIF-2α) agonist and its synergistic therapy with prolyl hydroxylase inhibitors for the treatment of renal anemia. Journal of Medicinal Chemistry 2021, 64 (23), 17384–17402. (cover) https://doi.org/10.1021/acs.jmedchem.1c01479
8. Yue Wu, Zhihong Li, Michael A. McDonough, Christopher J. Schofield, Xiaojin Zhang. Inhibition of the oxygen-sensing asparaginyl hydroxylase factor inhibiting hypoxia-inducible factor: A potential hypoxia response modulating strategy. Journal of Medicinal Chemistry 2021, 64 (11), 7189–7209. https://doi.org/10.1021/acs.jmedchem.1c00415
9. Pengfei Wang, Qijie Gong, Jiabo Hu, Xiang Li, Xiaojin Zhang. Reactive oxygen species (ROS)-responsive prodrugs, probes, and theranostic prodrugs: applications in the ROS-related diseases. Journal of Medicinal Chemistry 2021, 64 (1), 298–325. https://doi.org/10.1021/acs.jmedchem.0c01704
10. Xiaojin Zhang,* Yonghua Lei, Tianhan Hu, Yue Wu, Zhihong Li, Zhensheng Jiang, Changyong Yang, Lianshan Zhang, Qidong You.* Discovery of clinical candidate (5-(3-(4-chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an orally bioavailable prolyl hydroxylase inhibitor for the treatment of anemia. Journal of Medicinal Chemistry 2020, 63 (17), 10045–10060. https://doi.org/10.1021/acs.jmedchem.0c01161
11. Zhihong Li, Kaijun Su, Zhensheng Jiang, Yancheng Yu, Qidong You, Xiaojin Zhang. Photoactivatable prolyl hydroxylase 2 inhibitors for stabilizing the hypoxia-inducible factor with light. Journal of Medicinal Chemistry 2019, 62 (16), 7583–7588. (front cover) https://doi.org/10.1021/acs.jmedchem.9b00688
12. Zhihong Li, Qidong You, Xiaojin Zhang. Small-molecule modulators of the hypoxia-inducible factor pathway: Development and therapeutic applications. Journal of Medicinal Chemistry 2019, 62 (12), 5725–5749. https://doi.org/10.1021/acs.jmedchem.8b01596
13. Xingsen Wu, Xiang Li, Zhihong Li, Yancheng Yu, Qidong You, Xiaojin Zhang. Discovery of nonquinone substrates for NAD(P)H: quinone oxidoreductase 1 (NQO1) as effective intracellular ROS generators for the treatment of drug-resistant non-small cell lung cancer. Journal of Medicinal Chemistry 2018, 61 (24), 11280–11297. (cover) https://doi.org/10.1021/acs.jmedchem.8b01424
14. Yue Wu, Zhensheng Jiang, Zhihong Li, Jing Gu, Qidong You, Xiaojin Zhang. Click chemistry–based discovery of [3-hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as orally active hypoxia inducing factor prolyl hydroxylase inhibitors with favorable safety profiles for the treatment of anemia. Journal of Medicinal Chemistry 2018, 61 (12), 5332–5349. https://doi.org/10.1021/acs.jmedchem.8b00549