姓名:李佳 性别:男 职称:研究员 学历:博士 电话:0760-85286866 电子邮件:lijia@zidd.ac.cn 职务:院长,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
1992年毕业于浙江医科大学药学系。1994年进入中国科学院上海药物研究所攻读博士学位,2000年获理学博士学位。
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研究领域
代谢性疾病创新药物发现,代谢调控紊乱共性病理机制研究
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研究成果
已发现数百个新活性化合物,有20个1类候选新药进入系统临床前研究,其中13个候选1类新药实现转移转化,11个候选1类新药已经进入临床研究。已授权国际国内发明专利187项,申请86项。在Diabetes、Diabetologia、J Hepatology、Cell Res、Nat Commun、Leukemia、Cell Rep、Chem Soc Rev、Adv Mater、JACS、Angew Chem Int Ed、Chem Sci、JMC等国际期刊发表SCI论文570篇,其中通讯作者或者共同通讯作者文章293篇;影响因子总和超过3400;总引用超过14000次;h因子为57。
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代表性论著(*:通讯作者)
1. Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies. Liu Z, Jiang K, Liu Y, Li J, Huang S, Li P, Xu L, Xu X, Hu X, Zeng X, Huang Z, Zhou Y*, Li J*, Long K*, Wang M*. J Med Chem. 2024.
2. Discovery of potent PROTAC degraders of Pin1 for the treatment of acute myeloid leukemia. Shi Y, Liu M, Li M, Mao Y, Ma J, Long R, Xu M, Yang Y, Wang W*, Zhou Y*, Li J*, Zhou B*. Chem Sci. 2024; 15:5027.
3. Inulin-like polysaccharide ABWW may impede CCl4 induced hepatic stellate cell activation through mediating the FAK/PI3K/AKT signaling pathway in vitro & in vivo. Dai X, Du Z, Jin C, Tang B, Chen X, Jing X, Shen Y, He F, Wang S, Li J*, Ding K*, Zang Y*. Carbohydr Polym. 2024; 326:121637.
4. Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy. Cheng J, Yan Z, Jiang K, Liu C, Xu D, Lyu X, Hu X, Zhang S, Zhou Y*, Li J*, Zhao Y*. J Med Chem. 2023; 66(24):16991-7025.
5. Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader. Hu L, Li H, Qin J, Yang D, Liu J, Luo X, Ma J, Luo C, Ye F, Zhou Y*, Li J*, Wang M*. J Med Chem. 2023; 66(22):15269-87.
6. Anxiolytic effect of antidiabetic metformin is mediated by AMPK activation in mPFC inhibitory neurons. Zhang Y, Zong H, Qi Y, Chang L, Gao Y, Zhou T, Yin T, Liu M, Pan K, Chen W, Guo H, Guo F, Peng Y, Wang M, Feng L, Zang Y*, Li Y*, Li J*. Mol Psychiatry. 2023; 28(9):3955-65.
7. Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities. Li X, Wang P, Wang C, Jin T, Xu R, Tong L, Hu X, Shen L, Li J*, Zhou Y*, Liu T*. J Med Chem. 2023; 66(17):11792-814.
8. Dual inhibition of CHK1/FLT3 enhances cytotoxicity and overcomes adaptive and acquired resistance in FLT3-ITD acute myeloid leukemia. Jiang K, Li X, Wang C, Hu X, Wang P, Tong L, Tu Y, Chen B, Jin T, Wang T, Wang H, Han Y, Gui R, Yang J, Liu T*, Li J*, Zhou Y*. Leukemia. 2023; 37(3):539-49.
9. Targeting C/EBPα overcomes primary resistance and improves the efficacy of FLT3 inhibitors in acute myeloid leukaemia. Wang H, Luo G, Hu X, Xu G, Wang T, Liu M, Qiu X, Li J, Fu J, Feng B, Tu Y, Kan W, Wang C, Xu R, Zhou Y*, Yang J*, Li J*. Nat Commun. 2023; 14(1):1882.
10. Phosphorylation of PHF2 by AMPK releases the repressive H3K9me2 and inhibits cancer metastasis. Dong Y, Hu H, Zhang X, Zhang Y, Sun X, Wang H, Kan W, Tan M, Shi H*, Zang Y*, Li J*. Signal Transduct Target Ther. 2023; 8(1):95.
11. Orthogonally Engineered Albumin with Attenuated Macrophage Phagocytosis for the Targeted Visualization and Phototherapy of Liver Cancer. Dou W, Qiu P, Shi Y, Zhu L, Guo C, Li N, Zang Y, Liu T, Zhao S, Pan Y, Dong L, Sessler JL*, Tan Y*, Li J*, Wang H*, Tian H*, He X*. J Am Chem Soc. 2023; 145(31):17377-88.
12. Chloroquine enhances the efficacy of chemotherapy drugs against acute myeloid leukemia by inactivating the autophagy pathway. Wang H, Li J, Kan W, Xu G, Luo G, Song N, Wu W, Feng B, Fu J, Tu Y, Liu M, Xu R, Zhou Y*, Wei G*, Li J*. Acta Pharmacol Sin. 2023; 44(11):2296-306.
13. Hepatic glucuronyl C5-epimerase combats obesity by stabilizing GDF15. He F, Jiang H, Peng C, Wang T, Xiao R, Chen M, Song N, Du Z, Wang H, Ding X, Shao Y, Fang J, Zang Y, Hua R*, Li J*, Ding K*. J Hepatol. 2023; 79(3):605-17.
14. High-throughput screening of SARS-CoV-2 main and papain-like protease inhibitors. Zang Y, Su M, Wang Q, Cheng X, Zhang W, Zhao Y, Chen T, Jiang Y, Shen Q, Du J, Tan Q, Wang P, Gao L, Jin Z, Zhang M, Li C, Zhu Y, Feng B, Tang B, Xie H, Wang MW, Zheng M, Pan X, Yang H, Xu Y, Wu B, Zhang L, Rao Z, Yang X, Jiang H, Xiao G, Zhao Q*, Li J*. Protein Cell. 2023; 14(1):17-27.
15. Extracellular vesicles mediate antibody-resistant transmission of SARS-CoV-2. Xia B, Pan X, Luo R, Shen X, Li S, Wang Y, Zuo X, Wu Y, Guo Y, Xiao G, Li Q, Long X, He X, Zheng H, Lu Y, Pang W, Zheng Y*, Li J*, Zhang L*, Gao Z*. Cell Discov. 2023; 9(1):2.
16. Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition. Jiang K, Liu C, Nie L, Jiang H, Xu L, Zhang K, Fan L, Gao A, Lin L, Wang X, Tan M, Zhang Q, Zhou Y*, Li J*. Acta Pharmacol Sin. 2023; 44(1):234-243.
17. PD-L1/TLR7 dual-targeting nanobody-drug conjugate mediates potent tumor regression via elevating tumor immunogenicity in a host-expressed PD-L1 bias-dependent way. Yu X, Long Y, Chen B, Tong Y, Shan M, Jia X, Hu C, Liu M, Zhou J, Tang F, Lu H, Chen R, Xu P, Huang W, Ren J, Wan Y, Sun J, Li J*, Jin G*, Gong L*. J Immunother Cancer. 2022; 10(10):e004590.
18. Fluorescent probes for the detection of disease-associated biomarkers. Dou WT, Han HH, Sedgwick AC, Zhu G, Zang Y, Yang X*, Yoon J*, James TD*, Li J*, He X*. Sci Bull. 2022; 67(8):853-78.
19. Discovery of a Potent and Selective Degrader for USP7. Pei Y, Fu J, Shi Y, Zhang M, Luo G, Luo X, Song N, Mi T, Yang Y, Li J*, Zhou Y*, Zhou B*. Angew Chem Int Ed Engl. 2022; 61(33):e202204395.
20. Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. Zhang J, Che J, Luo X, Wu M, Kan W, Jin Y, Wang H, Pang A, Li C, Huang W, Zeng S, Zhuang W, Wu Y, Xu Y, Zhou Y*, Li J*, Dong X*. J Med Chem. 2022; 65(13):9096-9125.
21. Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis. Wang Q, Tang B, Sun D, Dong Y, Ji Y, Shi H, Zhou L, Yang Y, Luo M, Tan Q, Chen L, Dong Y, Li C, Xie R, Zang Y, Shen J, Xiong B, Li J*, Chen D*. Acta Pharm Sin B. 2022; 12(4):1943-1962.
22. Inner nuclear membrane protein TMEM201 promotes breast cancer metastasis by positive regulating TGFβ signaling. Kong Y, Zhang Y, Wang H, Kan W, Guo H, Liu Y, Zang Y*, Li J*. Oncogene. 2022; 41(5):647-656.
23. Downregulation of c-Myc expression confers sensitivity to CHK1 inhibitors in hematologic malignancies. Jiang K, Tong L, Wang T, Wang H, Hu X, Xu G, Jin T, Kan W, Xu L, Li J, Zhang K, Song N, Liu J, Zhang M, Wu W, Xiang Y, Gao A, Hu Y, Zhou Y*, Liu T*, Yang J*, Li J*. Acta Pharmacol Sin. 2022; 43(1):220-228.
24. Forrestiacids A and B, Pentaterpene Inhibitors of ACL and Lipogenesis: Extending the limits of Computational NMR Methods in the Structure Assignment of Complex Natural Products. Xiong J, Zhou P, Jiang H, Huang T, He Y, Zhao Z, Zang Y, Choo YM, Wang X, Chittiboyina AG, Pandey P, Hamann MT, Li J*, Hu JF*. Angew Chem Int Ed Engl. 2021; 60(41):22270-22275.
25. Small-molecule fluorescence-based probes for interrogating major organ diseases. Han H, Tian H, Zang Y, Sedgwick AC, Li J*, Sessler JL*, He X* James TD*. Chem Soc Rev. 2021; 50 (17):9391-9429.
26. SARS-CoV-2 envelope protein causes acute respiratory distress syndrome (ARDS)-like pathological damages and constitutes an antiviral target. Xia B, Shen X, He Y, Pan X, Liu FL, Wang Y, Yang F, Fang S, Wu Y, Duan Z, Zuo X, Xie Z, Jiang X, Xu L, Chi H, Li S, Meng Q, Zhou H, Zhou Y, Cheng X, Xin X, Jin L, Zhang H, Yu D, Li M, Feng X, Chen J, Jiang H, Xiao G, Zheng Y*, Zhang L*, Shen J*, Li J*, Gao Z*. Cell Res. 2021; 31(8):847-860.
27. DOT1L regulates thermogenic adipocyte differentiation and function via modulating H3K79 methylation. Shuai L, Li B, Jiang H, Yang L, Li J*, Li JY*. Diabetes. 2021; 70(6):1317-33.
28. Fluorescent probes for the imaging of lipid droplets in live cells. Tian H, Sedgwick AC, Han H, Sen S, Chen G, Zang Y, Sessler JL, James TD*, Li J*, He X*. Coord. Chem Rev. 2021; 427, 213577.
29. AMPK-mediated phosphorylation on 53BP1 promotes c-NHEJ. Jiang Y, Dong Y, Luo Y, Jiang S, Meng F, Tan M, Li J*, Zang Y*. Cell Rep. 2021; 34(7):108713.
30. Photochromic Fluorescent Probe Strategy for the Super-resolution Imaging of Biologically Important Biomarkers. Chai X, Han HH, Sedgwick AC, Li N, Zang Y, James TD, Zhang J*, Hu X, Yu Y, Li Y, Wang Y, Li J*, He X*, Tian H. J Am Chem Soc. 2020; 142(42):18005-18013.
31. Cyclodextrin-Based Peptide Self-Assemblies (Spds) That Enhance Peptide-Based Fluorescence Imaging and Antimicrobial Efficacy. Jiao J, Wang G, Hu X, Zang Y, Maisonneuve S, Sedgwick AC, Sessler JL*, Xie J*, Li J*, He X*, Tian H. J Am Chem Soc. 2020; 142(4):1925-1932.
32. Mitochondrial Uncoupling Coordinated With PDH Activation Safely Ameliorates Hyperglycemia Via Promoting Glucose Oxidation. Jiang H, Jin J, Duan Y, Xie Z, Li Y, Gao A, Gu M, Zhang X, Peng C, Xia C, Dong T, Li H, Yu L, Tang J, Yang F*, Li J*, Li J*. Diabetes 2019; 68(12):2197-2209.
33. SIRT5 Regulates Brown Adipocyte Differentiation and Browning of Subcutaneous White Adipose Tissue. Shuai L, Zhang L, Li B, Tang C, Wu L, Li J*, Li J*. Diabetes. 2019; 68(7):1449-1461.
34. Remote light-controlled intracellular target recognition by photochromic fluorescent glycoprobes. Zhang J, Fu Y, Han H, Zang Y, Li J*, He X*, Feringa BL, Tian H*. Nat Commun. 2017; 8(1):987.
35. Targeted Intracellular Production of Reactive Oxygen Species by a 2D Molybdenum Disulfide Glycosheet. Ji D, Zhang Y, Zang Y, Li J*, Chen G, He X*, Tian H. Adv Mater. 2016; 28(42):9356-9363.
36. Probing disease-related proteins with fluorogenic composite materials. He X, Zang Y, James TD, Li J*, Chen G*. Chem Soc Rev. 2015; 44(13):4239-4248.
37. A novel chemical uncoupler ameliorates obesity and related phenotypes in mice with diet-induced obese by modulating energy expenditure and food intake. Fu Y, Zhang M, Turner N, Zhang L, Dong T, Gu M, Leslie SJ, Li J*, Nan F*, Li J*. Diabetologia. 2013; 56(10):2297-2307.
38. Fluorogenic probing of specific recognitions between sugar ligands and glycoproteinreceptors on cancer cells by an economic graphene nanocomposite. Zhang H, Wei X, Cao J, Liu S, He X*, Chen Q, Long Y, Li J*, Chen G*, Chen K. Adv Mater. 2013; 25(30):4097-101.
39. High-throughput assay for modulators of mitochondrial membrane potential identifies a novel compound with beneficial effects on db/db mice. Qiu B, Turner N, Li Y, Gu M, Huang M, Wu F, Pang T, Nan F, Ye J, Li J*, Li J*. Diabetes. 2010; 59:256-65.
40. Berberine, and its more biologically available derivative dihydroberberine, inhibit mitochondrial respiratory complex I: a mechanism for the action of berberine to activate AMPK and improve insulin action. Turner N, Li J, Gosby A, To S, Cheng Z, Miyoshi H, Taketo M, Cooney G, Kraegen E, David J, Hu L*, Li J*, Ye J*. Diabetes. 2008; 57:1414-18.