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高 剑，副教授，博士，硕士生导师 |
科学研究方向 |
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糖尿病、肿瘤等重大疾病防治药物的计算机辅助药物设计，药物合成与活性评价 |
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联系方式 |
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电 话：0516-83262137 |
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Email：gaojian@xzhmu.edu.cn |
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通 讯：江苏省徐州市云龙区铜山路209号，221004 |
个人简历
中国科学院大学化学生物学博士(2013年)，副教授，硕士生导师，药物化学学科后备带头人。江苏省“青蓝工程”优秀青年骨干教师（2019年），江苏省“六大人才高峰”高层次人才（2019年）。主持国家自然科学基金青年项目，江苏省自然科学基金面上项目，江苏省自然科学基金青年项目，徐州市科技计划项目，徐州医科大学优秀人才科研启动基金等各1项。近年来，以第一作者或者通讯作者，在Signal Transduct Tar (IF: 38.104, 2022), P. Natl. Acad. Sci. USA (IF: 12.779, 2021), Cell. Commun. Signal. (IF: 7.525, 2022), Nanoscale (IF: 7.394, 2014), Eur. J. Med. Chem. (IF: 7.088, 2019, 2022), Front. Pharmacol. (IF: 5.988, 2021), Front. Mol. Biosci. (IF: 6.113, 2021), Mol. Med. (IF: 6.376, 2022), Int. J. Mol. Sci. (IF: 4.556, 2016, 2019), J. Comput.-Aided Mol. Des. (IF: 3.25, 2018, 2019)等SCI收录期刊发表论文30余篇。申请国家发明专利9项，授权8项。
承担科研课题
1. 国家自然科学基金青年项目，21708033，基于Sirt1激动机制的全新激动剂发现及其在糖尿病肾病药物防治中的应用，2018.01-2020.12，22万元，主持。
2. 江苏省自然科学基金面上项目，BK20201157，2-甲基萘并[1,2-b]呋喃类Sirt1 激动剂的设计、合成及其抗糖尿病肾病活性评价，2020.07-2023.06，10万元，主持。
3. 江苏省自然科学基金青年项目，BK20140225，基于人PDF的新型抗肿瘤药物设计，2014.06-2017.07，20万元，主持。
4. 徐州市科技创新专项-高校基础研究，KC16SG249，基于人肽脱甲酰基酶的新型抗肿瘤药物设计，2016.10-2018.10，5万元，主持。
5. 徐州医科大学优秀人才科研启动基金，D2014008，靶向人肽脱甲酰基酶的新型抗肿瘤药物设计，2014.05-2017.05，30万元，主持。
6. 横向课题：中国医学科学院阜外医院，靶向α7nAChR的全新药物分子筛选，2020.10-2021.10，7万元，主持。
指导本科生获得省级以上科研项目或竞赛
1. 第八届全国大学生基础医学创新研究暨实验设计论坛总决赛铜奖。基于结构发现甘草黄酮B和银杏黄酮靶向c-Myc G-四链体对c-Myc转录和骨髓瘤生长的抑制作用。唯一指导教师。
2. 2022全国大学生生命科学竞赛一等奖。CULSC2022CY0265，曲伐沙星，奥扎莫德和奥泽沙星靶向c-Myc G-四联体的计算机辅助药物设计及活性研究。唯一指导教师。
3. 2021全国大学生生物科学竞赛江苏赛区三等奖。JS-CULSC2021KS01，基于SIRT1激活剂白藜芦醇的生物信息学分析与计算机辅助药物设计。唯一指导教师。
4. 2019第十六届“瑞华杯”江苏省大学生课外学术科技作品竞赛暨“挑战杯”全国竞赛江苏省选拔赛决赛二等奖。靶向SIRT1的糖尿病肾病防治的计算机辅助药物设计。唯一指导教师。
5. 2018年第十一届“全国大学生药苑论坛”创新成果奖一等奖。唯一指导教师。
6. 2016年第一届全国医药院校药学/中药学大学生创新创业暨实验教学改革大赛获得特等奖。NDC16A110002059，个人排名：4/5。
7. 2022年国家级大学生创新创业训练计划项目。基于Omomyc的全新靶向c-Myc的抗肿瘤多肽的计算机辅助药物设计，202210313018Z，1万元，唯一指导教师。
8. 2021年国家级大学生创新创业训练计划项目。蛋白Myc/Max/Omomyc与DNA分子间互作的计算机辅助药物设计，202110313022Z，1万元，唯一指导教师。
9. 2019年国家级大学生创新创业训练计划项目。基于白藜芦醇的全新SIRT1激活剂的计算机辅助药物设计，201910313005Z，1万元，唯一指导教师。
10. 2016年国家级大学生创新创业训练计划项目。基于中草药的新型抗菌药物发现，201610313014Z，1万元，唯一指导教师。
授权国家发明专利
1. 高剑，林奇泗，牟杰，王涛，朱亚胜，邱圣智，梁礼。香草醛异羟肟酸类衍生物及其应用，ZL201611103571 .3
2. 高剑，姚若斯。一种2-亚胺苯并咪唑类化合物及医药用途，ZL201811390517 .0
3. 高剑，姚若斯。吡咯烷-2-酮类化合物在制备与多发性骨髓瘤有关药物方面的应用，ZL202011215542 .2
4. 印晓星，高剑，鲁茜，周成华，姚若斯，杜蕾，陈庆庆。2-甲基萘并[1 ,2-b]呋喃类化合物在制备与糖尿病肾病有关药物方面的应用，ZL 201911119378 .2
5. 刘泳，高剑，底洁卉，郑骏年，王丙武。靶向MDM2锌指结构域的小分子药物及其抗肿瘤用途，ZL 201910552173 .7
6. 姚若斯，高剑。咪唑并喹唑啉类衍生物及其盐制备PIM1酶抑制剂的应用、PIM1酶抑制剂及其应用，ZL 201911070051 .0
7. 周雪妍，郭晓莉，高剑，印晓星，张蓓，徐吟。一种靶向ACSL1的小分子药物及其在治疗子宫内膜癌中的应用，ZL 202110902537 .7
8. 邱净英，龚奇能，谷小珂，陈旺，高剑，黄健航。一种丙烯酰胺类化合物、其制备方法及医药用途，ZL201710127451 .5
近五年代表性论文、专著
1. [中科院1区top, IF: 38.104] Yu Zhenlong#, Gao Jian#, Zhang Xiaolei#, Peng Yulin#, Wei Wenlong, Xu Jianrong, Li Zhenwei, Wang Chao, Zhou Meirong, Tian Xiangge, Feng Lei, Huo Xiaokui, Liu Min, Ye Mingliang*, Guo De-an*, Ma Xiaochi*. Characterization of a small-molecule inhibitor targeting NEMO/IKKβ to suppress colorectal cancer growth. Signal Transduction and Targeted Therapy 2022; 7(1): 71.
2. [中科院1区top, IF: 12.779] Yuan Wei#, Lu Liaoxun#, Rao Muding, Huang Yang, Liu Chun-e, Liu Shuang, Zhao Yue, Liu Huicong, Zhu Jiangli, Chao Tianzhu, Wu Can, Ren Junyan, Lv Luxian, Li Wenqiang, Qi Shiqian, Liang Yinming, Yue Shijing, Gao Jian*, Zhang Zhongjian#, Kong Eryan*. GFAP hyperpalmitoylation exacerbates astrogliosis and neurodegenerative pathology in PPT1-deficient mice. Proc Natl Acad Sci U S A 2021; 118(13): e2022261118.
3. [中科院1区top, IF: 7.088] Qiu Jingying, Zhou Qingqing, Zou Yueting, Li Shuqiong, Yang Lihua, Chen Wang, Gao Jian*, Gu Xiaoke*. Design and synthesis of novel quinazolinone derivatives as anti-HBV agents with TLR8 agonist effect. Eur J Med Chem 2022; 231: 114159.
4. [中科院1区top, IF: 5.572] Qiu Jingying#, Chen Wang#, Zhang Yinpeng, Zhou Qingqing, Chen Jing, Yang Lihua, Gao Jian*, Gu Xiaoke*, Tang Daoquan*. Assessment of quinazolinone derivatives as novel non-nucleoside hepatitis B virus inhibitors. Eur J Med Chem 2019; 176: 41-49.
5. [中科院1区top, IF: 7.394]Gao Jian, Wang Liming, Kang Seung-gu, Zhao Lina, Ji Mingjuan*, Chen Chunying, Zhao Yuliang, Zhou Ruhong, Li Jingyuan*. Size-dependent impact of CNTs on dynamic properties of calmodulin. Nanoscale 2014; 6(21): 12828-12837.
6. [中科院2区top, IF: 5.998] Gao Jian, Chen Qing-Qing, Huang Ye, Li Kai-Hang, Geng Xiao-Ju, Wang Tao, Lin Qi-Si*, Yao Ruo-Si*. Design, Synthesis and Pharmacological Evaluation of Naphthofuran Derivatives as Potent SIRT1 Activators. Front Pharmacol 2021; 12(917): 653233.
7. [中科院2区, IF: 7.525] Yao Ruosi#, Zhang Menghui#, Zhou Jian, Liu Linlin, Zhang Yan, Gao Jian*, Xu Kailin*, Novel Dual-Targeting C-Myc Inhibitor D347-2761 Represses Myeloma Growth Via Blocking C-Myc/Max Heterodimerization and Disturbing Its Stability. Cell Communication and Signaling 2022, 20(1):73.
8. [中科院2区, IF: 6.376] Wang Bingwu#, Gao Jian#, Zhao Zhongjun#, Zhong Xuefei, Cui Hao, Hou Hui, Zhang Yanping, Zheng Junnian*, Di Jiehui*, Liu Yong*. Identification of a small-molecule RPL11 mimetic that inhibits tumor growth by targeting MDM2-p53 pathway. Mol Med 2022; 28(1): 109.
9. [中科院2区, IF: 3.841] Geng, Xiaoju#, Yan Zhang#, Shihao Li, Linlin Liu, Ruosi Yao*, Ling Liu, Jian Gao*. Design, synthesis, and biological evaluation of novel benzimidazolyl isoxazole derivatives as potential c-Myc G4 stabilizers to suppress c-Myc transcription and myeloma growth', J Mol Struct 2023; 1275: 134673.
10. [中科院2区, IF: 4.556] Chen Qingqing#, Wang Yan#, Shi Shanshan, Li Kaihang, Zhang Ling, Gao Jian*. Insights into the Interaction Mechanisms of the Proviral Integration Site of Moloney Murine Leukemia Virus (Pim) Kinases with Pan-Pim Inhibitors PIM447 and AZD1208: A Molecular Dynamics Simulation and MM/GBSA Calculation Study. International Journal of Molecular Sciences 2019; 20(21): 5410.
11. [中科院2区, IF: 3.226] Gao Jian*, Liang Li, Zhu Yasheng, Qiu Shengzhi, Wang Tao, Zhang Ling. Ligand and Structure-Based Approaches for the Identification of Peptide Deformylase Inhibitors as Antibacterial Drugs. International Journal of Molecular Sciences 2016; 17(7): 1141.
12. [中科院3区, IF: 6.113] Qu Zhiyuan, Li Kaihang, Geng Xiaoju, Huang Bo, Gao Jian*. Computational Insights Into the Effects of the R190K and N121Q Mutations on the SARS-CoV-2 Spike Complex With Biliverdin. Frontiers in Molecular Biosciences 2021; 8(1189): 791885.
13. [中科院3区, IF: 2.552] Shi Shanshan#, Wang Qiudan#, Liu Sai, Qu Zhiyuan, Li Kaihang, Geng Xiaoju, Wang Tao, Gao Jian*. Characterization the performances of twofold resveratrol integrated compounds in binding with SIRT1 by molecular dynamics simulation and molecular mechanics/generalized born surface area (MM/GBSA) calculation. Chem Phys 2021; 544: 111108.
14. [中科院3区, IF: 4.162] Yao R. S., Xie Y., Sun X. Y., Zhang M. H., Zhou J., Liu L. L., Gao J.*, Xu K. L.* Identification of a Novel c-Myc Inhibitor 7594-0037 by Structure-Based Virtual Screening and Investigation of Its Anti-Cancer Effect on Multiple Myeloma. Drug Des Dev Ther 2020; 14: 3983-3993.
15. [中科院3区, IF: 2.546] Chen Han, Wang Yan, Gao Zheng, Yang Wen, Gao Jian*. Assessing the performance of three resveratrol in binding with SIRT1 by molecular dynamics simulation and MM/GBSA methods: the weakest binding of resveratrol 3 to SIRT1 triggers a possibility of dissociation from its binding site. J Comput-Aided Mol Des 2019; 33(4): 437-446.
16. [中科院3区, IF: 2.535] Yao Ruosi#, Sun Xiaoyang#, Xie Yu, Sun Xiaoshen, Yao Yao, Li Hujun, Li Zhenyu, Gao Jian*, Xu Kailin*. Identification of a novel c-Myc inhibitor with anti-tumor effects on multiple myeloma cells. Biosci Rep 2018: BSR20181027.
17. [中科院3区, IF: 3.25] Gao Jian#,*, Liang Li#, Chen Qingqing, Zhang Ling, Huang Tonghui*. Insight into the molecular mechanism of yeast acetyl-coenzyme A carboxylase mutants F510I, N485G, I69E, E477R, and K73R resistant to soraphen A. J Comput-Aided Mol Des 2018; 32(4): 547-557.
18. [中科院3区, IF: 2.861] Gao Jian*, Wang Tao, Qiu Shengzhi, Zhu Yasheng, Liang Li, Zheng Youguang. Structure-Based Drug Design of Small Molecule Peptide Deformylase Inhibitors to Treat Cancer. Molecules 2016; 21(4): 396.
19. [中科院4区, IF: 4.05] Zhang Jinyuan#, Wang Tao#, Geng Xiaoju, Liu Linlin, Gao Jian*, Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent C-Myc G-Quadruplex Stabilizers to Suppress C-Myc Transcription and Myeloma Growth. Mol inform 2022:e2200011.
20. [中科院4区, IF: 2.817] Liu Linlin#, Geng Xiaoju#, Zhang Jinyuan, Li Shihao, Gao Jian*, Structure-Based Discovery of Licoflavone B and Ginkgetin Targeting C-Myc G-Quadruplex to Suppress C-Myc Transcription and Myeloma Growth. Chem. Biol. Drug Des. 2022. https://doi.org/10.1111/cbdd.14064.
21. [中科院4区, IF: 2.172] Gao Jian#,*, Wang Yinchuan#, Li Kaihang, Zhang Jinyuan, Geng Xiaoju. Comparative analysis of compound NSC13728 as Omomyc homodimer stabilizer by molecular dynamics simulation and MM/GBSA free energy calculation. J Mol Model 2022; 28(4): 92.
22. [中科院4区, IF: 1.965] An Yiqiang#, Meng Chen#, Chen Qingqing, Gao Jian*. Discovery of small molecule sirt1 activator using high-throughput virtual screening, molecular dynamics simulation, molecular mechanics generalized born/surface area (MM/GBSA) calculation, and biological evaluation. Med Chem Res 2020; 29(2): 255-261.
23. [中科院4区, IF: 1.783] Liu Linlin, Kai Xiaoning, Chen Qingqing, Zhang Ling, Yao Ruosi*, Gao Jian*. Identification of protein arginine methyltransferase 7 (PRMT7) inhibitor by virtual screening and biological evaluation in vitro. Med Chem Res 2019; 28(2): 125-132.
24. [中科院4区, IF: 1.728] Shi Xi, Zhang Yan, Qiu Shiwei, Zhuang Wei, Yuan Na, Sun Tiantian, Gao Jian*, Qiao Yuehua*, Liu Ke*. A Novel GJB2 compound heterozygous mutation c.257C>G (p.T86R)/c.176del16 (p.G59A fs*18) causes sensorineural hearing loss in a Chinese family. J Clin Lab Anal 2018; 32(7): e22444.
25. [中科院4区, IF: 1.2] Jian Gao, Shengzhi Qiu, Li Liang, Zhixiang Hao, Qianqian Zhou, Fanfan Wang, Jie Mou*, Qisi Lin*. Design, Synthesis, and Biological Evaluation of Vanillin Hydroxamic Acid Derivatives as Novel Peptide Deformylase Inhibitors. Curr Comput Aided Drug Des 2018; 14(1): 95-101.
26. [中科院4区, IF: 1.503] Li Liang, Qianqian Zhou, Zhixiang Hao, Fanfan Wang, Yasheng Zhu, Qisi Lin*, Jian Gao*. The discovery of antibacterial natural compound based on peptide deformylase. Combinatorial Chem High Throughput Screening 2018; 21(4): 292-297.
27. [中科院4区, IF: 1.607] Gao Jian#, Sun Jie#, Wang Tao, Sheng Shen, Huang Tonghui*. Combined 3D-QSAR modeling and molecular docking study on spiro-derivatives as inhibitors of acetyl-CoA carboxylase. Med Chem Res 2017; 26(2): 361-371.
