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中国科学院上海药物研究所导师教师师资介绍简介-赵玉军

本站小编 Free考研考试/2021-02-10

xm:赵玉军
xb:男
zc:研究员
xl:博士
dh:
cz:
dzyj:yjzhao@simm.ac.cn
grzy:
zjlb:研究员;新药;
zw:研究组长
txdz:上海市浦东新区海科路501号4号楼604室
grjj:赵玉军, 中国科学院上海药物研究所研究员,课题组长。2003年本科毕业于江苏省苏州大学化学化工学院,2019年研究生毕业于新加坡南洋理工大学获有机化学博士学位,2009-2015 年在美国密西根大学癌症中心从事博士后研究。主要从事的激酶和蛋白质相互作用小分子抑制剂的设计合成、及生物活性研究。先后研究了蛋白相互作用MDMX/p53抑制剂、BFL1/BH3抑制剂、BET-Bromodomain/Histone抑制剂、TEAD/YAP1抑制剂,NIK、ASK1、EGFR等激酶抑制剂作为靶向药物分子。以通讯作者或第一作者在Cancer Cell, J. Am. Chem. Soc., J. Med. Chem., FASEB J., Eur. J. Med. Chem.等国际重要学术刊物发表论文30余篇;申请PCT专利7项、中国专利11项,获中国授权发明专利3项、获美国授权发明专利8项;主持“重大新药创制”科技重大专项、国家自然科学基金面上项目、中国科学院战略性先导专项(A类)等多项省部级以上重点科研项目。


yjfx:1. 蛋白之间相互作用的小分子抑制剂研究;
2.小分子激酶抑制剂的药物化学研究;
3. 天然产物结构改造及药物化学性质研究。
dblz:1.Zhiqiang Li+, Xinzhi Li+, Ming-Bo Su+, Li-Xin Gao, Yu-Bo Zhou, Bingchuan Yuan, Xilin Lyu, Ziqin Yan, Chujiao Hu, Hao Zhang, Cheng Luo, Zheng Chen*, Jia Li*, Yujun Zhao*, Discovery of a potent and selective NF-κB-inducing kinase (NIK) inhibitor that has anti-inflammatory effects in vitro and in vivo, Journal of Medicinal Chemistry, 2020, 63, 4388-4407. (+equal contributions)

2.Shiyan Zhang, Chaoying Huang, Xilin Lyu,+ Peipei Wang, Yi Zang, Zengtao Wang, Huan Wang, Jia Li*, Yujun Zhao*, Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal -regulating kinase 1 (ASK1), European Journal of Medicinal Chemistry, 2020, 195, 112277.

3.Deheng Chen, Tian Lu, Ziqin Yan, Wenchao Lu, Feilong Zhou, Xilin Lyu, Biling Xu, Hualiang Jiang, Kaixian Chen, Cheng Luo*, and Yujun Zhao*, Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins, European Journal of Medicinal Chemistry, 2019, 182, 111633.

4.Erbao Zhao, Feilong Zhou, and Yujun Zhao*, Lewis Acids Promoted 3+2 Cycloaddition of Oxaziridines and Cyclic Allylic Alcohols through Carbonyl Imine Intermediates, Journal of Organic Chemistry, 2019, 84 (7), 4282–4293.

5.Deheng Chen, Dexiang Guo, Ziqin Yan, Yujun Zhao*, Allenamide as a bioisostere of acrylamide in design andsynthesis of targeted covalent inhibitors Med. Chem. Commun. 2018, 9, 244-253.

6.Feilong Zhou, Erbao Zhao, Ziqin Yan, Deheng Chen, Yujun Zhao*, Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles, Tetrahedron Letters, 2018, 59, 1871-1874.

7.Xiaomeng Ren, Xinzhi Li, Linna Jia, Deheng Chen, Hai Hou, Liangyou Rui, Yujun Zhao*, Zheng Chen*, A small-molecule inhibitor of NF-kB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury, FASEB Journal. 2017, 2, 711-718.

申请和授权专利:

1.赵玉军,周飞龙, 严子琴, 一种具有苄氧基芳环结构的化合物,其制备方法和用途, 中国专利申请号: 8.5,申请日期: 2019-06-04;

2.赵玉军,王欢,周飞龙, 严子琴,吕细林,具有2H-吲唑结果的小分子化合物及其合成和应用,中国专利申请号: 3.7, 申请日期: 2019-03-06

3.赵玉军、李佳、王增涛、张世言、臧奕、王培培、孙丹丹、张含烟, 2-吡啶取代脲结构小分子化合物及其合成和应用,中国专利申请号: 0.X, 申请日期: 2019-08-05

4.赵玉军、陈德恒、郭德祥、严子琴、周飞龙、耿美玉、丁健、沈爱军、刘红椿、张敏敏,一种BRD4 抑制剂及其制备和应用, 中国专利申请公布号: 1 .1, 申请公布日期: 2018-04-13;

5.赵玉军,李志强,严子琴,李佳,周宇波,苏明波,陈政,一种具有2-氨基嘧啶结构的化合物,其制备方法和用途,中国专利申请号: 9.0,申请日期: 2018-11-20;

6.赵玉军、郭德祥、严子琴,含有共轭联烯酰胺结构的化合物、其制备方法、药物组合物和用途, 中国专利号: ZL6.8, 申请日期: 2017-11-10;

7.赵玉军、陈德恒、严子琴,含有共轭联烯结构的化合物、其药物组合物和用途, 中国专利申请号: 3.0, 申请日期: 2017-07-31.


jyjl:苏州大学,化学师范,学士
新加坡国立大学,有机化学,博士肄业新加坡南洋理工大学,有机化学,博士
gzjl: 新加坡南洋理工大学,Research Officer 美国密西根大学癌症中心,博士后 中国科学院上海药物科学研究所,研究员
ktxm:中国科学院战略性先导专项(A类),项目四、子课题29,XDA**,新颖ASK1激酶抑制剂的设计、合成及活性研究,86.05万,在研,主持。国家自然科学基金委员会,面上项目,**,设计合成新颖的MAP3K14激酶抑制剂和降解剂,研究其生物活性和成药性,57.00万,在研,主持。“重大新药创制”科技重大专项, 子课题名称:基于蛋白翻译后修饰调控的新药研究关键技术, 2018ZX**-004-010, 开发新颖的NIK抑制剂调控IKKα磷酸化和p100降解,研究其成药性, 115.73万,在研,主持。国家自然科学基金委员会,面上项目,**,BET-Bromodomain小分子抑制剂和BET蛋白降解剂的设计合成及其表观遗传学性质研究,59.00万,在研,主持。
ryhj:
xpwj:http://sourcedb.simm.cas.cn/zw/gb2020/yjzz/202008/P.jpg
kycg:1.Discovery of small molecule BY27 that blocks BET bromodomain/Histone protein-protein interactions: our data demonstrated significant differences between a selective BET BD2 inhibitor and a pan BET inhibitor, which suggest that selective BET BD2 inhibitors have potential pharmaceutical applications in clinical setting.

2.Discovery of a selective NIK kinase inhibitor XT2: our data show that small molecule NIK inhibitor XT2 inhibited that activation of NFκB2 signal pathway in liver cells, decreased the liver cells apoptosis induced by toxin, and prolonged the life span of mice in a liver-damage model. These results suggest that inhibition of NIK activity in vivo maybe a good therapeutic target for treating liver-damage related diseases.

3.Discovery of a selective ASK1 kinase inhibitor YD57: our data show that YD57 inhibited ASK1 and several other kinases, which promoted apoptosis, induced cell cycle arrest, and had very potent activities in killing liver cancer cells.

4.Discovery of EGFR kinase inhibitors: we found that the allenamide moiety was a good bioisostere of the acrylamide group in structures of covalent EGFR inhibitors. The allenamide moiety reacted with the -SH group of a cysteine much faster than that of the acrylamide group. These data suggest the allenamide moiety could be used for labeling the -SH group of cysteines in vitro and in intact cells.


shrz:
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