江余祺

作者:蔡超时间:2019-10-21

江余祺

博士

副教授

硕士生导师

室:

药物合成研究室

办公电话:

0532-85902675

电子邮箱:

jiangyuqi@ouc.edu.cn

联系地址:

山东省青岛市香港东路23中国海洋大学浮山校区C220

研究方向:

1. 基于氨肽酶N/CD13的靶向抗肿瘤药物的研究

2. 新型NLRP3炎症小体抑制剂的设计与开发

3. 利用ProTide前药技术开发多功能核苷类抗肿瘤药物

个人简介

 

 

 

 

主要从事氨肽酶N/CD13的靶向抗肿瘤药物的研究,以及新型NLRP3炎症小体抑制剂的设计、合成及作用机制的研究。近五年来,在Med Res Rev, J Med Chem, Eur J Med Chem, ACS Chem Neurosci等杂志发表SCI论文20余篇,申请国内外专利5项,3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”创新药物重大专项等课题。

教育背景

 

 

 

 

2011.09~2016.12

山东大学药学院

药物化学

博士

2007.09~2011.06

山东大学药学院

药学

学士

工作经历

 

 

 

 

2019.07~至今

中国海洋大学医药学院

副教授

 

2016.05~2019.07

美国弗吉尼亚联邦大学药学院

博士后

 

学术兼职

中国药学会会员

担任J. Med. Chem., Eur. J. Med. Chem., Chem Biol Drug Des审稿人

承担课程

 

 

 

 

药物化学(本科生课程)

药物化学实验(本科生课程)

高等药物化学(研究生课程)

研究进展

 

 

 

 

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。

代表性成果

代表性论文

 

 

 

 

1.      Jakob C Green#, Yuqi Jiang#, Liu He, YimingXu, 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. (共同第一作)

2.      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. (共同第一作者)

3.      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, 97189731. 亮点报道,Molecules 2020, 25, 119

4.      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(3): 777-790.

5.      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.

6.      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.

7.      Yuqi Jiang, Jingnin Hou, Xiaoyang Li, Yongxue Huang, Xuejian Wang, Jingde Wu, Jian Zhang, WenfangXu, Yingjie Zhang*. Discovery of a Novel Chimeric Ubenimex-Gemcitabine with Potent Oral Antitumor Activity. Bioorg Med Chem. 2016, 24(22):5787-5795.

8.      Yuqi Jiang, Xiaoyang Li, Xue Wang, Zhonglan Wang, Jian Zhang, Jingde Wu*, Wenfang Xu*. Design, Synthesis, Biological Chracterization of Tamibarotene Analogs as Anticancer Agents. Chem Biol Drug Des, 2016, 4(88): 542-555.

9.      Yuqi Jiang, Xiaoguang Li, Xiaoyang Li, Jinning Hou, Yongzheng Ding, Jian Zhang, Wenfang Xu* and Yingjie Zhang*. Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU. Med Chem, 2016, 12(1): 30-6.

10.  Yuqi Jiang, Jinning Hou, Xiaoyang Li, Wenfang Xu* and Yingjie Zhang*. Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent. Lett Drug Des Discov, 2016, 13(8):729-733.

11.  Jacob Fulp, Liu He, Stefano Toldo, Yuqi Jiang, Ashley Boice, Chunqing Guo, Xia Li, Andrew Rolfe, Dong Sun, Antonio Abbate, Xiang-Yang Wang, Shijun Zhang*. Structural Insights of Benzene Sulfonamide Analogs as Nlrp3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2018, 61, 5412-5423.

12.  Xiaoyang Li#, Yingjie Zhang*#, Yuqi Jiang, Jingde Wu, Elizabeth S. Inks, C. James Chou, Shuai Gao, Jinning Hou, Qinge Ding, Jingyao Li, Xue Wang, Yongxue Huang, Wenfang Xu. Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. Eur J Med Chem. 2017; 134:185-206.

13.  Chunqing Guo#, Jacob W. Fulp#, Yuqi Jiang, Xia Li, Jeremy E. Chojnacki, Jingde Wu, Xiang-Yang Wang*, Shijun Zhang*. Development and Characterization of a Hydroxyl-Sulfonamide Analogue,5-Chloro-N-[2-(4-Hydroxysulfamoyl-Phenyl)-Ethyl]-2-Methoxy-Benzamide, as a Novel Nlrp3 Inflammasome Inhibitor for Potential Treatment of Multiple Sclerosis. ACS Chem Neurosci.2017, 8, 2194-2201.

14.  Lei Zhang*, Yantao Han, Qixiao Jiang, Chunbo Wang, Xuehong Chen, Xiaoguang Li, Fuming Xu, Yuqi Jiang, Qiang Wang, Wenfang Xu. Trend of Histone Deacetylase Inhibitors in Cancer Therapy: Isoform Selectivity or Multitargeted Strategy. Med Res Rev. 2015, 35, 63-84.

15.  Xiaoyang Li, Elizabeth S. Inks, Xiaoguang Li, Jinning Hou, C. James Chou, Jian Zhang, Yuqi Jiang, Yingjie Zhang*and Wenfang Xu*. Discovery of the first N-hydroxycinnamamide -based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity.J Med Chem. 2014; 57(8):3324-3334.

16.  Xiaoyang Li,Jinning Hou, Xiaoguang Li, Yuqi Jiang, Xueliang Liu, Weiwei Mu, YimingJin, Yingjie Zhang*, Wenfang Xu*. Development of 3-Hydroxy cinnamamide-Based HDAC Inhibitors with Potent in vitro and in vivo Anti-tumor Activity. Eur J Med Chem. 2015; 7(89):628-637.

17.  Liu He, Yuqi Jiang, Jakob Green, Hallie Blevins, Shijun Zhang*. Development of bivalent compounds as potential neuroprotectants for Alzheimers disease. Bioorg Med Chem Lett. 2019,29(15):1957-1961.

18.  Ram Kuwar, Andrew Rolfe, Long Di, Hongyu Xu, Liu He, Yuqi Jiang, Shijun Zhang, and Dong Sun*. A novel small molecular NLRP3 inflammasome inhibitor alleviates neuroinflammatory response following traumatic brain injury. J Neuroinflammation. 2019; 16(1):81-95.

19.  Xin Liu, Zhihua Zhang, Yuqi Jiang, Yue Hu, Zhonglan Wang, Junli Liu, Ruihua Feng, Jie Zhang, Guihua Huang*. Novel PEG-grafted nanostructured lipid carrier for systematic delivery of a poorly soluble anti-leukemia agent Tamibarotene: characterization and evaluation. Drug Deliv. 2015, 22(2):223-229.

专利

 

 

 

 

1.      Wenfang Xu, Yuqi Jiang, Yingjie Zhang, Mingming Zou, Jinning Hou, Jin Li, Xuejian Wang,XiaoyangLi. Multi-targeted Ubenimex Prodrug Derivative And Preparation Method And Use Thereof. US:2018.01.09 JP:2017.12.27 EP:2018.09.26, US9861703B2,JP6254264B2, EP 2947070B2, WO2014194848A1. 美国,日本,欧洲(英国、德国、法国、瑞士)。

2.      Wenfang Xu; Jian Zhang; Yuqi Jiang; Xiaobo Xu; Xiaoyang Li; Leqiao Tan; Yongxue Huang; Xuejian Wang; Multifunctional immunity-targeted micromolecule anti-cancer medicine bestazomib (Bestazomib) and preparation method and application thereof, 2019-8-05, WIPO, PCT/CN2019/099305

3.      徐文方,江余祺,邹明明。多靶点型乌苯美司前药衍生物及其制备方法和用途. 2014.09.17, 中国,CN103588713B

4.      张颖杰,徐文方,江余祺李晓杨,侯金宁,丁永正. 多靶点型他米巴罗汀衍生物及其制备方法和应用. 2015.12.03, 中国,CN10517528A

5.      吴敬德, 王雪,曲颖,江余祺李晓杨. 一种以 Raf/MEK/ERK PI3K/Akt为靶点的双通道抑制剂. 2016.08.10, 中国,CN10394858B

项目课题

  1. 1. 国家自然科学基金青年科学基金项目,820035842021-2023,在研,主持。

  2. 2. 中国海洋大学“青年英才工程”第三层次科研基金2019-2024,在研,主持。

  3. 3. 中国海洋大学院士基金子课题2019-2022,在研,主持。

  4. 4. 山东省重大科技创新工程专项(2018SDKJ0403), 在研,参与。

    5. 山东省重点研发计划(2020CXGC010503,在研,参与。






 

 

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