微生物与生化药学——药物化学方向

李卓荣

来源:    

作者:    

时间:2021-07-02    

浏览次数:


李卓荣   研究员   博士生导师

教育背景及工作经历:1983年北京医学院药物化学专业本科毕业,1988年北京协和医学院微生物药物学研究生毕业。1992年至1994年,日本东京北里研究所研修;1997年至1999年,美国Oklahoma大学访问学者。现任中国医学科学院医药生物技术研究所研究员、博士生导师、学系副主任等。

主要研究方向:药物设计、合成与构效关系研究及新药研发

专业研究领域:专业领域为药物化学,主要研究方向包括抗菌、抗病毒、抗肿瘤及抗骨质疏松等药物的分子设计、构效关系研究与新药研发。先后负责主持国家自然科学基金、“863”计划课题、重大新药创制等国家科技项目十多项,牵头主持十二五重大新药创制化学药临床前研究课题。作为主要成员,参加国家自然科学基金委创新群体、重大新药创制综合大平台及品种课题、比尔盖茨基金会重大课题等多项。多年来,在国内外学术刊物上发表研究论文160多篇。通讯/并列通讯作者论文在AutophagyHepatologyPhytomedicine J. Med. Chem Eur J Med. Chem.ACS Infectious DiseasesBioorgan Med ChemFront NeurosciFront PharmacolJ Alzheimers Dis.Fututre Medicinal ChemistryMolecular oncologyLife SciActa Pharmaceutica Sinica BMoleculesRSC AdvancesCancer Chemotherapy & PharmacologyTetrahedron Letter等刊物发表。与企业合作开展新药品种的研发,临床研究中1类新药1项,临床前2项。

代表性论文:

1. Dai-Jie Chen,,* A-Long Cui,,* Jia-Rong Chen, Ping Yang, Jie Jin, Lei Shao, and Zhuo-Rong Li. The Low-Alkalinity Polymyxin Derivative, AL-6, Shows High Activity Against Multidrug-Resistant Acinetobacter baumannii Clinical Isolates In Vitro and A. baumannii ATCC 19606 In Vivo: Preliminary Analysis of the Antibacterial Mechanism. Microbial Drug Resistance, 2021. DOI: 10.1089/mdr.2019.0474.

2. Xinyue Hu, Hailun Jang, Weiqi Bai, Xiujun Liu, Qingfang Miao, Linlin Wang, Jie Jin, Along Cui, Rui Liua*, and Zhuorong Li*. Synthesis, characterization, and targeted chemotherapy of SCT200-linker-monomethyl auristatin E conjugates. Eur J Med Chem. 2021, 216:113297.

3. Si-tu Xue, Ke Li, Yang Gao, Lu-yao Zhao, Yan Gao, Hong Yi, Jian-dong Jiang*, and Zhuo-rong Li*. The role of the key autophagy kinase ULK1 in hepatocellular carcinoma and its validation as a treatment target. Autophagy, 2020, 16:10, 1823-1837.

4. Xinbei Jiang, Jiali Tan, YixuanWang, Jinhua Chen, Jianrui Li, Zhi Jiang, Yanni Quan, Jie Jin, Yuhuan Li, Shan Cen, Yanping Li*, Zonggen Peng*, Zhuorong Li*. 2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as OrallyAvailable Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action. Journal of Medicinal Chemistry. 2020; 63(11):5972-5989.

5. Si-tu Xue, Lei Zhang, Zhuo-song Xie, Jie Jin, Hui-Fang Guo, Hong Yi, Zong-ying Liu**, Zhuo-rong Li*. Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, antiosteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties. European Journal of Medicinal Chemistry, 2020, 200:112465.

6. A-Long Cui, Xin-Xin Hu, Yang Chen, Jie Jin, Hong Yi, Xiu-Kun Wang, Qi-Yang He, Xue-Fu You*, Zhuo-Rong Li*. Design, Synthesis, and Bioactivity of Cyclic Lipopeptide Antibiotics with Varied Polarity, Hydrophobicity, and Positive Charge Distribution. ACS Infectious Diseases, 2020, 6(7):1796-1806.

7. Jing Geng, Yuhong Wang, Lei Zhang, Co Li, Weijin Sheng*, Zhuorong Li*, Min Jiang1. The Cajanine Derivative LJ101019C Regulates the Proliferation and Enhances the Activity of NK Cells via Kv1.3 Channel-Driven Activation of the AKT/mTOR Pathway. Phytomedicine, 2020, 66:153113.

8. Hailun Jiang, Li Zeng, Xueqi Dong, Shuilong Guo, Jianguo Xing, Zhuorong Li*, Rui Liu*. Tilianin Extracted From Dracocephalum moldavica L. Induces Intrinsic Apoptosis and Drives Inflammatory Microenvironment Response on Pharyngeal Squamous Carcinoma Cells via Regulating TLR4 Signaling Pathways. Front Pharmacol, 2020; 11: 205.

9. Wang Linlin#, Fang Jiansong#, Jiang Hailun, Wang Qian, Xue Situ, Li Zhuorong*, Liu Rui*. 7-pyrrolidinethoxy-4'-methoxyisoflavone prevents amyloid β–induced injury by regulating histamine H3 receptor-mediated cAMP/CREB and AKT/GSK3β pathways. Front Neurosci, 2019, 13:334.

10. Wang Linlin#, Liu Jianghong#, Wang Qian, Jiang Hailun, Zeng Li, Li Zhuorong*, Liu Rui*. MicroRNA-200a-3p mediates neuroprotection in Alzheimer-related deficits and attenuates amyloid-beta overproduction and tau hyperphosphorylation via coregulating BACE1 and PRKACB. Front Pharmacol, 2019, 10:806.

11. Xin-yue Hu, Rong Wang, Jie Jin, Xiu-jun Liu, A-long Cui, Lian-qi Sun, Yan-ping Li, Yi Li, Yu-cheng Wang, Yong-su Zhen, Qing-fang Miao*, Zhuo-rong Li*. An EGFR-Targeting Antibody-Drug Conjugate LR004-VC-MMAE: Potential in Esophageal Squamous Cell Carcinoma and Other Malignancies. Molecular oncology, 2019; 13(2):246-263.

12. A-Long Cui, Xin-Xin Hu, Yan Gao, Jie Jin, Hong Yi, Xiu-Kun Wang, Tong-Ying Nie, Yang Chen, Qi-Yang He, Hui-Fang Guo, Jian-Dong Jiang, Xue-Fu You*, Zhuo-Rong Li*. The Synthesis and Bioactivity Investigation of the Individual Components of Cyclic Lipopeptide Antibiotics. Journal of Medicinal Chemistry, 2018, 61, 1845-1857.

13.Xing-Yue Ji, Jin-Hua Chen, Guang-Hui Zheng, Meng-Hao Huang, Lei Zhang, Hong Yi, Jie Jin, Jian-Dong Jiang, Zong-Gen Peng*, Zhuo-Rong Li*. Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. J Med Chem, 2016, 59(22):10268-10284.

14. Zong-Gen Peng, Zhi-Yun Zhao, Yan-Ping Li, Yu-Ping Wang, Lan-Hu Hao, Bo Fan, Yu-Huan Li, Yue-Ming Wang, Yong-Qiang Shan, Yan-Xing Han, Yan-Ping Zhu, Jian-Rui Li, Xue-Fu You, Zhuo-Rong Li*, Jian-Dong Jiang*. Host Apolipoprotein B Messenger RNA-Editing Enzyme Catalytic Polypeptide-Like 3G Is an Innate Defensive Factor and Drug Target Against Hepatitis C Virus. Hepatology, 2011, 53 (4): 1080-1089.

15. Hui-fang Guo†, Hua-yi Shao†, Zhao-yong Yang†, Si-tu Xue, Xue Li, Zong-ying Liu, Xiao-bo He, Jian-dong Jiang, Yue-qin Zhang, Shu-yi Si* and Zhuo-rong Li*. Substituted Benzothiophene or Benzofuran Derivatives as a Novel Class of Bone Morphogenetic Protein-2 Up-Regulators: Synthesis, Structure-Activity Relationships, and Preventive Bone Loss Efficacies in SAMP6 and Ovariectomized Rats. Journal of Medicinal Chemistry, 2010; 53, 1819-1829.

专利:获得中国专利证书20多个,美国、欧洲、日本、香港等国际授权5

专著:参与编写《抗病毒药物及其研究方法》(第二版)

荣誉奖励:国务院特贴专家和卫健委突贡专家,北京协和医学院教学名师、师德模范等。2019年获得中国药学会生物医药创新奖。

学术任职:担任药学领域多个专业协会委员或期刊编委:中国药学会生化与生物技术专业委员会委员、中国药学会药物化学专业委员会委员、中国生化制药协会多肽药物分会专家委员会委员等;《Acta Pharmacentica Sinica B》《药学学报》《中国抗生素杂志》《中国医药生物技术杂志》编委等。

联系电话:010-83152017

电子邮箱:lizhuorong@imb.pumc.edu.cn