张晓进

来源:赵飞发布时间:2022-09-15浏览次数:8238

 


张晓进,博士,教授,博士生导师,理学院化学系主任。英国牛津大学(University of Oxford)化学系访问学者(2019-2020)。江苏省杰出青年基金(2021)、江苏省优秀青年基金(2017)获得者,江苏省“333高层次人才培养工程”中青年科技领军人才(2022)。

 

主持国家、省级科研项目7项。以通讯作者在药物化学领域国际著名刊物Journal of Medicinal Chemistry、European Journal of Medicinal Chemistry等发表SCI论文50余篇;已授权中国发明专利7项、欧洲专利1项、日本专利1项。曾获国家科技进步奖二等奖(2016)、江苏省科学技术一等奖(2015)、中国药学会-施维雅青年药物化学奖(2016)。作为主要负责人之一设计研发的抗肾性贫血1类新药在中国进入临床II期试验。

 

研究生招生专业:药物化学(博士)、药物化学(学硕)、药学-制药化学(专硕)

研究生招生方向:临床需求导向的靶向药物分子设计、合成及成药性研究

主要研究方向:围绕细胞“氧感知通路”及“氧化还原系统”开展靶向新药研发及化学生物学研究

实验室常用技术手段:计算机辅助药物分子设计,化学合成与结构表征,靶标及细胞水平的生物活性评价,动物水平的安全性与药效学评价,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C409

 

近年代表性论文:

1.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. (supplementary cover)

2.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.

3.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.

4.Yancheng Yu, Quanwei Yu, Simeng Liu, Chenyang Wu, Xiaojin Zhang.* Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation. European Journal of Medicinal Chemistry 2021, 211, 112999.

5.Qijie Gong, Fulai Yang, Jiabao Hu, Pengfei Wang, Tian Li, Xiang Li,* Xiaojin Zhang.* Rational designed highly sensitive NQO1-activated near-infrared fluorescent probe combined with NQO1 substrates in vivo: an innovative strategy for NQO1-overexpressing cancer theranostics. European Journal of Medicinal Chemistry 2021, 224, 113707.

6.Qijie Gong, Quanwei Yu, Nan Wang, Jiabao Hu, Pengfei Wang, Fulai Yang, Tian Li, Qidong You,* Xiang Li,* Xiaojin Zhang.* Application of cation-π interactions in enzyme-substrate binding: design, synthesis, biological evaluation, and molecular dynamics insights of novel hydrophilic substrates for NQO1. European Journal of Medicinal Chemistry 2021, 221, 11351.

7.Qijie Gong, Jiabao Hu, Pengfei Wang, Xiang Li,* Xiaojin Zhang.* A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials. European Journal of Medicinal Chemistry 2021, 210, 112962.

8.Kaijun Su, Zhihong Li, Yancheng Yu, Xiaojin Zhang.* The prolyl hydroxylase inhibitor roxadustat: Paradigm in drug discovery and prospects for clinical application beyond anemia. Drug Discovery Today 2020, 25 (7), 1262–1269.

9.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.

10.Zhihong Li, Shuai Zhen, Kaijun Su, Anthony Tumber, Quanwei Yu, Ying Dong, Michael McDonough, Christopher J. Schofield,* Xiaojin Zhang.* A small-molecule probe for monitoring binding to prolyl hydroxylase domain 2 by fluorescence polarisation. Chemical Communications 2020, 56 (91), 14199–14202

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)

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.

13.Yancheng Yu, Quanwei Yu, Xiaojin Zhang.* Allosteric inhibition of HIF-2α as a novel therapy for clear cell renal cell carcinoma. Drug Discovery Today 2019, 24 (12), 2332−2340.

14.Zhensheng Jiang, Qidong You,* Xiaojin Zhang.* Medicinal chemistry of metal chelating fragments in metalloenzyme active sites: A perspective. European Journal of Medicinal Chemistry 2019, 165, 172−197.

15.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. (supplementary cover)

16.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.

17.Xian Zhang, Xiang Li, Zhihong Li, Xingsen Wu, Yue Wu, Qidong You,* Xiaojin Zhang.* An NAD(P)H: quinone oxidoreductase 1 responsive and self-immolative prodrug of 5-fluorouracil for safe and effective cancer therapy. Organic Letters 2018, 20 (12), 3635−3638.

18.Jinlei Bian, Xiang Li, Nan Wang, Xingsen Wu, Qidong You,* Xiaojin Zhang.* Discovery of quinone-directed antitumor agents selectively bioactivated by NQO1 over CPR with improved safety profile. European Journal of Medicinal Chemistry 2017, 129, 27−40.

19.Jinlei Bian, Xiang Li, Lili Xu,Nan Wang, Xue Qian, Qidong You,* Xiaojin Zhang.* Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. European Journal of Medicinal Chemistry 2017, 127, 828−839.

20.Xian Zhang, Xiang Li, Qidong You,* Xiaojin Zhang.* Prodrug strategy for cancer cell-specific targeting: a recent overview. European Journal of Medicinal Chemistry 2017, 139, 542−563.