个人简介
副教授,硕士生导师。2019年加入中国海洋大学医药学院开展独立工作,入选中国海洋大学“青年英才工程”第三层次。主要从事氨肽酶N/CD13、HDAC的靶向抗肿瘤药物的研究,新型NLRP3炎症小体抑制剂的设计与开发,以及核苷类抗肿瘤药物研究。近五年来,在Med Res Rev, J Med Chem, Eur J Med Chem等杂志发表SCI论文30余篇,申请国内外专利7项,4项已被授权,主持并参与国家自然科学基金、山东省重大科技创新工程、国家科技部“十二五”创新药物重大专项、企业横向等课题,获青岛市科技进步二等奖。
教育背景
2011~2016 山东大学药学院 药物化学 医学博士
2007~2011 山东大学药学院 药学 理学学士
工作经历
2019~至今 中国海洋大学医药学院 副教授
2016~2019 美国弗吉尼亚联邦大学药学院 博士后
学术兼职
中国药学会高级会员
担任Eur J Med Chem, Chem Biol Drug Des, Drug Development Research等杂志审稿人
研究领域
(1)、氨肽酶N (APN/CD13)是一类Zn2+ 依赖的II型跨膜蛋白酶,在肿瘤细胞表面及新生血管、基质中高表达。CD13的生物学功能主要有三方面:水解多肽、内吞的细胞膜蛋白受体和信号传导分子,因此,CD13是与肿瘤的侵袭转移、新生血管生成、免疫调节等多方面相关的靶点,同时,CD13是肝癌干细胞表面标志物,与肝癌的发生、耐药和复发密切相关。因此,CD13是肿瘤靶向治疗的重要靶点。细胞毒类化疗药如5-氟尿嘧啶、阿霉素、吉西他滨等,在临床化疗时往往会引起肿瘤细胞CD13的表达上调而产生耐药。CD13抑制剂乌苯美司与抗癌化疗药联合用药,能增强疗效,逆转耐药,降低不良反应的发生率。因此开发基于CD13的新型多靶点多功能抗肿瘤药物具有重要的价值。目前,主要开展靶向CD13的新型偶联药物的研究。
(2)、炎症小体是新近发现的一类大分子复合体,对机体的免疫系统具有重要的调节作用。在众多炎症小体中,NLRP3炎症小体是目前研究最为清楚的,它的异常激活与多种疾病密切相关,如冷吡啉相关周期性综合症、痛风、阿尔兹海默症、类风湿性关节炎、动脉粥样硬化、炎症性肠炎、非酒精性脂肪肝等。因此,开发安全、有效的炎症小体抑制剂对于NLRP3-相关疾病的临床治疗有重要的意义。目前,主要开展基于NLRP3蛋白结构的合理药物设计。
近期论文
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Liang Zhang, Kangjing Qi, Jie Xu, Yan Xing, Xuejian Wang, Ling Tong, Zengguo He, Wenfang Xu, Xiaoyang Li*, and Yuqi Jiang*, Design, synthesis and anti-cancer evaluation of novel cyclic phosphate prodrug of gemcitabine. J Med Chem. 2023, in press.
Yuqi Jiang#, Jie Xu#, Kairui Yue#, Chao Huang, Mengting Qin, Dongyu Chi, Qixin Yu, Yue Zhu, Xiaohan Hou, Tongqiang Xu, Min Li, C. James Chou*, and Xiaoyang Li*, Potent hydrazide-based HDAC inhibitor with superior pharmacokinetic profile for efficient treatment of acute myeloid leukemia in vivo.J Med Chem. 2022,65, 285-302.
Jakob C Green#, Yuqi Jiang#, Liu He, Yiming Xu, Sun Dong, Timothy Keoprasert, Christopher Nelson, Unsong Oh, Edward J Lesnefsky, Glen E Kellogg, Qun Chen, Shijun Zhang*. Characterization and discovery of a selective small molecule modulator of mitochondrial complex I targeting a unique binding site. J Med Chem. 2020, 63, 11819-11830. (co-first author)
Xiaoyang Li*#, Yuqi Jiang#, Yuri K. Peterson, Tongqiang Xu, Richard A. Himes, Xin Luo, Guilin Yin, Elizabeth S. Inks, Nathan Dolloff, Stephanie Halene, Sherine S. L. Chan, and C. James Chou*. Design of hydrazide-bearing HDACIs based on panobinostat and their p53 and FLT3-ITD dependency in anti-leukemia activity. J Med Chem. 2020, 63, 5501-5525. (co-first author)
Yuqi Jiang, Liu He, Jakob C. Green, Hallie Blevins, Chunqing Guo, Sulay Patel, Matthew Sean Halquist, MaryPeace McRae, Jurgen Venitz, Xiang-Yang Wang, and Shijun Zhang*.Discovery of second-generation NLRP3 inflammasome inhibitors: Design, synthesis, and biological characterization.J Med Chem. 2019, 62, 9718−9731. (Highlighted in Molecules 2020, 25, 119)
Liu He, Yuqi Jiang, Kai Liu, Victoria Gomez-Murcia, Xiaopin Ma, Alejandro Torrecillas, Qun Chen, Xiongwei Zhu, Edward Lesnefsky, Juan C. Gomez-Fernandez, Bin Xu, Shijun Zhang*. Insights into the Impact of a Membrane-Anchoring Moiety on the Biological Activities of Bivalent Compounds as Potential Neuroprotectants for Alzheimer's Disease. J Med Chem. 2018, 61, 777-790.
Kairui Yue#, Xiaohan Hou#, Geng Jia, Liang Zhang, Jian Zhang, Leqiao Tan, Xuejian Wang, Zhaolin Zhang, Peixia Li, Wenfang Xu, Xiaoyang Li*, Yuqi Jiang*. Design, synthesis and biological evaluation of hybrid of ubenimex-fluorouracil for hepatocellular carcinoma therapy, Bioorg Chem, 2021, 116, 105343.
Yuqi Jiang, Xiaoyang Li, Jinning Hou, Yongxue Huang, Xuejian Wang, Yuping Jia, Qingwei Wang, Wenfang Xu, Jian Zhang*, Yingjie Zhang*. Synthesis and Biological Characterization of Ubenimex-Fluorouracil Conjugates for Anti-Cancer Therapy. Eur J Med Chem. 2018, 143, 334-347.
Yuqi Jiang, Xiaoyang Li, Jinning Hou, Yongxue Huang, Yuping Jia, Mingming Zou, Jian Zhang, Xuejian Wang*, Wenfang Xu*, Yingjie Zhang*. Discovery of BC-01, a novel mutual prodrug (hybrid drug) of ubenimex and fluorouracil as anticancer agent. Eur J Med Chem. 2016, 121, 649-657.
Yuqi Jiang, Jingnin Hou, Xiaoyang Li, Yongxue Huang, Xuejian Wang, Jingde Wu, Jian Zhang, Wenfang Xu, Yingjie Zhang*. Discovery of a Novel Chimeric Ubenimex-Gemcitabine with Potent Oral Antitumor Activity. Bioorg Med Chem. 2016, 24, 5787-5795.