姓名：李翼 性别：男 职称：研究员 学历：博士 电话：0760-85286866 电子邮件：liyi@simm.ac.cn 职务：课题组长 通讯地址：广东翠亨新区中瑞（欧）工业园健康医药示范区
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个人简历
李翼博士，2009年本科毕业于武汉大学药学院，同年保送至中国科学院上海药物研究所硕博连读，2014年获药物化学博士学位，随后留所工作。2016年，入选上海药明康德“Young Talent Program”，在国内新药研发部从事小分子创新药物研发，期间作为项目药化负责人，负责多个新药项目从立项、临床前研究、IND开发到临床申报工作。2018年赴美，在美国德克萨斯大学医学分部从事博士后研究。获中国科学院院长奖，赛诺菲-中科院上海生命科学院优秀博士后奖等荣誉。
2022年加入中科中山药物创新研究院，担任研究员、课题组长、博士生导师。
研究领域
1.抗肿瘤和代谢性疾病的创新药物研发；
2.基于药物优势骨架的有机合成新方法研究。研究成果
主要针对恶性肿瘤和代谢性疾病开展小分子创新药物研发，同时以药物分子的优势骨架为导向进行有机不对称合成方法学研究。新药研发方面，作为项目药化负责人和专利主要发明人，已成功完成4个候选新药的临床前研发和临床试验申报（IND）工作；基础研究方面，主要针对表观遗传调控蛋白，转录因子和蛋白激酶等重要靶标，开展药物化学研究，并发展了一系列构建高光学纯度手性胺类化合物和含季碳手性杂环类化合物的有机不对称合成方法。
迄今为止，已在J. Med. Chem., ACS Catal. Org. Lett., Chem. Comm.等国际权威药物化学和有机化学学术期刊上发表学术论文共24篇（第一和共同第一作者13篇），累计总影响因子大于140，总他引次数超过450次；申请或授权发明专利15项（13项为PCT专利）；撰写英文专著2章。多个研究成果发表后受到国际同行的关注和好评，其中6篇被德国化学评论期刊Synfacts作为亮点报道， 4篇被选为期刊封面文章，1篇被ChemComm推荐为Editor’s Choice，1篇被选为ACS Catal.期刊首页推荐文章。代表性论著（*：通讯作者）
1. Z. Liu#, Y. Li#, H. Chen, H.-T. Lai, P. Wang, S.-Y. Wu, E. A. Wold, P. G. Leonard, S. Joseph, H. Hu, C.-M. Chiang, A. R. Brasier*, B. Tian*, J. Zhou*, Discovery, X-ray Crystallography, and Anti-Inflammatory Activity of Bromodomain-Containing Protein 4 (BRD4) Inhibitors Targeting a Distinct New Binding Site, J. Med. Chem. 2022, 65, 2388-2408. (Selected as the Special Issue “Epigenetics 2022” and Cover Article)
2. Y. Li#, J. Chen#, A. Bolinger, H. Chen, Z. Liu, Y. Cong, A. R. Brasier, I. V. Pinchuk, B. Tian*, J. Zhou*, Target-Based Small Molecule Drug Discovery towards Novel Therapeutics for Inflammatory Bowel Diseases, Inflamm. Bowel Dis. 2021, 27, S38–S62.
3. Y. Li, M. Xu*, Applications of Asymmetric Petasis Reaction in the Synthesis of Chiral Amines, Acta Chim. Sinica 2021, 79, 1345.
4. Y. Li#, Z. Liu#, G. Aglyamova#, J. Chen, H. Chen, M. Bhandari, M. A. White, G. Rudenko⁎, J. Zhou⁎, Discovery of Phenanthridine Analogues as Novel Chemical Probes Disrupting the Binding of DNA to ΔFosB Homodimers and ΔFosB/JunD Heterodimers, Bioorg. Med. Chem. Lett. 2020, 30, 127300.
5. Y. Li#, B. Liu#, M. Xu*, Rhodium-Catalyzed Enantioselective Alkenylation of Cyclic Ketimines: Synthesis of Multifunctional Chiral α,α-Disubstituted Allylic Amine Derivatives, Org. Lett. 2018, 20, 2306. (Highlighted by Synfacts, 2018, 14, 0596)
6. Y. Li#, Y. Yu#, M. Xu*, Simple Open-Chain Phosphite-Olefin as Ligand for Rh-Catalyzed Asymmetric Arylation of Cyclic Ketimines: Enantioselective Access to gem-Diaryl α-Amino Acid Derivatives, ACS Catal. 2016, 6, 661. (Highlighted by The Journal Homepage).
7. H. Wang#, Y. Li#, M. Xu*, Rhodium-Catalyzed Highly Enantioselective Arylation of Cyclic Diketimines: Efficient Synthesis of Chiral Tetrasubstituted 1,2,5-Thiadiazoline 1,1-Dioxides, Org. Lett. 2014, 16, 3962. (Highlighted by Synfacts, 2014, 10, 1044)
8. Y. Li, M. Xu*, Rhodium-Catalyzed Asymmetric Tandem Cyclization for Efficient and Rapid Access to Underexplored Heterocyclic Tertiary Allylic Alcohols Containing a Tetrasubstituted Olefin, Org. Lett. 2014, 16, 2712. (Highlighted by Synfacts, 2014, 10, 0680)
9. Y. Li, M. Xu*, Simple Sulfur-Olefins as New Promising Chiral Ligands for Asymmetric Catalysis, Chem. Commun. 2014, 50, 3771. (Feature Article, Selected as Cover Article)
10. Y. Li, D. Zhu, M. Xu*, A new Versatile Approach to Enantioenriched 3-Hydroxyoxindoles, 1, 3-Dihydroisobenzofuran and 3-Isochromanone Derivatives by Rhodium-Catalyzed Asymmetric Arylation/Cyclization Sequence, Chem. Commun. 2013. 49, 11659. (Highlighted by Synfacts, 2014, 10, 0285; ChemComm Editor’s Choice)
11. Y. Li, M. Xu*, Lewis Acid-Catalyzed Intramolecular Aza-Friedel-Crafts Reaction of N-tert-Butanesulfinyl Imines: Efficient Synthesis of Optically Active 9-Aminoflourene Derivatives, Asian J. Org. Chem. 2013, 2, 50-53. (Selected as Cover Article; One of the most-accessed Asian J. Org. Chem. articles in April 2013)
12. Y. Li, M. Xu*, Lewis Acid-Promoted Highly Diastereoselective Petasis Borono-Mannich Reaction: Efficient Synthesis of Optically Active β, γ-Unsaturated α-Amino Acids, Org. Lett. 2012, 14, 2062. (Highlighted by Synfacts, 2012, 8, 0744)
13. Y. Li, D. Ji, M. Xu*, Highly Diastereoselective Friedel-Crafts Reaction of Arenes with N-tert-Butanesulfinylimino Ester towards the Efficient Synthesis of α-Arylglycines, Org. Biomol. Chem. 2011, 9, 8452.
14. J. Chen, Y. Li, C. Liu, T. Wang, L. W. Chung, M. Xu*, Water as Direct Proton Source for Asymmetric Hydroarylation Catalyzed by a Rh(I)-Diene: Concise Access to Non-proteinogenic β2/γ2/δ2-Amino Acid Derivatives, Org. Lett. 2021, 23, 571. (Highlighted by Synfacts, 2021, 17, 0462)
15. X. Xu, M. Mann, D. Qiao, Y. Li, J. Zhou, A. R. Brasier*, Bromodomain Containing Protein 4 (BRD4) Regulates Inducible Expression of Its Interactome in the Innate Response to Respiratory Syncytial Virus, Front. Mol. Biosci. 2021, 8, 728661.
16. X. Wang, T. Qiu, Y. Wu, C. Yang, Y. Li, G. Du, Y. He, W. Liu, R. Liu, C. Chen, Y. Shi, J. Pan, J. Zhou, D. Jiang*, C. Chen*, Arginine Methyltransferase PRMT5 Methylates and Stabilizes KLF5 via Decreasing Its Phosphorylation and Ubiquitination to Promote Basal Like Breast Cancer, Cell Death Differ. 2021, 28, 2931.
17. M. Mann, D. S. Roberts, Y. Zhu, Y. Li, J. Zhou, Y. Ge, A. R. Brasier*, Discovery of RSV-induced BRD4 Protein Interactions Using Native Immunoprecipitation and Parallel Accumulation—Serial Fragmentation (PASEF) Mass Spectrometry, Viruses 2021, 13, 454. (Special Issue Next-Generation Technologies to Understand Mechanisms of Virus Infections)
18. Z. Liu, H. Chen, P. Wang, Y. Li, E. A. Wold, P. G. Leonard, S. Joseph, A. R. Brasier*, B. Tian*, J. Zhou*, Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation, J. Med. Chem. 2020, 63, 5242. (Selected as the Cover Article)
19. X. Zhang*, X. Sheng, J. Shen, S. Zhang, W. Sun, C. Shen*, Y. Li, J. Wang, H. Lv, M. Cui, Y. Zhu, L. Huang, D. Hao, Z. Qi, G. Sun, W. Mao, Y. Pan, L. Shen, X. Li, G. Hu, Z. Gong, S. Han, J. Li, S. Chen, R. Tu, X. Wang, C. Wu, Discovery and Evaluation of Pyrazolo[3,4 d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor, ACS Med. Chem. Lett. 2020, 11, 1863.
20. T. Yu*, N. Li, C. Wu, A. Guan, Y. Li, Z. Peng, M. He, J. Li, Z. Gong, L. Huang, B. Gao, D. Hao, J. Sun, Y. Pan, L. Shen, C. Chan, X. Lu, H. Yuan, Y. Li, J. Li, S. Chen, Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR, ACS Med. Chem. Lett. 2018, 9, 256.
21. J. Chen, W. Chen, Y. Li, M. Xu*, A Highly Diastereoselective Friedel–Crafts Reaction of Indoles with Isatin-Derived N-Sulfinyl Ketimines towards the Efficient Synthesis of Chiral Tetrasubstituted 3-Indolyl-3-Aminooxindoles, Org. Biomol. Chem. 2015, 13, 3363.
22. T. Wang, W. Chen, Y. Li, M. Xu*, Facile Synthesis of Acridines via Pd(0)-Diphosphine Complex-Catalyzed Tandem Coupling/Cyclization Protocol, Org. Biomol. Chem. 2015, 13, 6580.
23. J. Wu, Y. Li, K. Chen, H. Jiang, M. Xu*, D. Liu*, Identification of Benzofuran-3-yl(phenyl)methanones as Novel SIRT1 Inhibitors: Binding Mode, Inhibitory Mechanism and Biological Action, Eur. J. Med. Chem. 2013, 60, 441.
24. L. Chen, Y. Li, M. Xu*, One-pot Synthesis of Furocoumarins via Sequential Pd/Cu-Catalyzed Alkynylation and Intramolecular Hydroalkoxylation, Org. Biomol. Chem. 2010, 8, 3073.
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