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个人简介：李佳，男，现任中国科学院上海药物研究所 研究员、博士生导师、课题组长、国家新药筛选中心模型建立部主管。1992 年毕业于浙江医科大学药学系。 2000 年在中国科学院上海药物研究所获理学博士学位。同年 8 月工作于国家新药筛选中心，负责高通量药物筛选模型的建立。2003 年应邀访问英国剑桥大学病理系参与细胞凋亡和新生血管生成相关研究。2004 年 8 月至 2005 年 2 月作为访问学者应邀赴澳大利亚 Garvan 医学研究所从事糖尿病相关合作研究。主要从事的研究工作包括：围绕糖尿病、神经退行性疾病、肿瘤等重大疾病，系统化克隆、表达、纯化和基因转染相关分子靶点，建立分子家族筛选平台和疾病靶向组合筛选模型平台；通过高通量筛选发现先导化合物；研究先导化合物和靶标相互作用模式；结合 RNA 干扰技术和化学生物学方法开展活性化合物作用机制研究和新靶点研究。承担和参与多项国家和上海市的重大科学研究项目。近五年已在国际杂志发表论文 45 篇，其中以通讯作者身份在Diabetes, J. Biol. Chem., J. Med. Chem., ChemBioChem 等杂志发表论文22篇。申请中国和国际专利 42项。作为第五完成人曾分获 2002 年度上海市科技进步一等奖和 2003 年度国家科技进步二等奖。
研究领域：
蛋白激酶、蛋白酪氨酸磷酸酯酶、蛋白水解酶、去乙酰化酶结构、功能及小分子调节剂研究；新型抗糖尿病先导化合物发现；中草药及天然产物（Berberine等）作用机制研究及化学生物学方法研究新型药物作用靶点。
专业业绩：
参与或承担多项“973”项目、“863”项目、自然科学基金项目、中国科学院知识创新工程战略行动计划重大项目、中国科学院知识创新工程重要方向项目、上海市重大、重点项目。
近三年发表论文（*：通讯作者；IF：影响因子）：
Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells. Pang T, Zhang ZS, Gu M, Qiu BY, Yu LF, Cao PR, Shao W, Su MB, Li JY, Nan FJ*, Li J*. J Biol Chem 2008, in press. (IF: 5.808)
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 JY, Gosby A, To S, Cheng Z, Miyoshi H, Taketo M, Cooney G, Kraegen E, David J, Hu LH*, Li J*, Ye JM*. Diabetes 2008, in press. (IF: 7.955)
5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside induces astroglial differentiation of neural stem cells via activating JAK/STAT3 pathway independently on AMP-activated protein kinase. Zang Y, Yu LF, Pang T, Fang LP, Feng X, Wen TQ, Nan FJ, Feng LY, Li J*. J. Biol. Chem. 2008, 283:6201-6208. (IF: 5.808)
Corosolic acid stimulates glucose uptake via enhancing insulin receptor phosphorylation. Shi L, Zhang W, Zhou YY, Zhang YN, Li JY, Hu LH, Li J*. Eur. J Pharmacol. 2008, accepted. (IF: 2.522)
Design, Synthesis, and Biological Evaluation of Caprolactam-Modified Bengamide Analogues. Liu G, Ma YM, Tai WY, Xie CM, Li YL, Li J*, Nan FJ*. ChemMedChem 2008, 3:73-78.
Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening. Shi L, Yu HP, Zhou YY, Du JQ, Shen Q, Li JY, Li J*. Acta Pharmacol. Sin. 2008, 29:278-284. (IF: 1.397)
Anti-Helicobacter pylori and Thrombin Inhibitory Components from Chinese Dragon’s Blood Dracaena cochinchinensis. Zhu YD, Zhang P, Yu HP, Li J*, Wang MW*, Zhao WM*. J Nat. Prod. 2007, 70:1570-1577. (IF: 2.418)
Benzoquinones from Ardisia japonica with Inhibitory Activity towards Human Protein Tyrosine Phosphatase 1B (PTP1B). Li YF, Li J, Shen Q, Hu LH. Chem. Biodivers. 2007, 4:961-965. (IF: 1.616)
Two New Coumarins from Fraxinus chinensis Rexb. Zhang DM, Wang LL, Li J, Hu LH. Journal of Integrative Plant Biology 2007, 49:218-221. (IF: 0.515)
Activity-based protein profiling for type I methionine aminopeptidase by the use of photo-affinity tri-modular probes. Qiu WW, Xu J, Li JY, Li J*, Nan FJ*. ChemBioChem 2007, 8:1351-1358. (IF: 4.1)
Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors. Zhang L, Qiu BY, Xiong B, Li X, Li JY, Wang X, Li J*, Shen JK*. Bioorg. Med. Chem. Lett. 2007, 17:2118-2122. (IF: 2.538)
Novel irreversible caspase-1 inhibitor attenuates the maturation of intracellular IL-1β. Ma XQ, Zhang HJ, Zhang YH, Wu F, Chen YH, Du JQ, Yu HP, Zhou ZL, Li JY, Nan FJ*, Li J*. Biochem. Cell Biol. 2007, 85:56-65. (IF: 3.483)
Conserved alpha helix act as autoinhibitory sequence in AMP-activated protein kinase alpha subunits. Pang T, Xiong B, Li JY, Qiu BY, Jin GZ, Shen JK, Li J*. J Biol. Chem. 2007, 282:495-506. (IF: 5.808)
Vascular development is disrupted by endothelial cell-specific expression of the antiapoptotic protein Bcl-2. Duval H, Johnson N, Li J, Evans A, Chen S, Licence D, Skepper J, Charnock-Jones DS, Smith S, Print C. Angiogenesis 2007, 10:55-68.
Preparation of 6-substituted quinoxaline JSP-1 inhibitors by microwave accelerated nucleophilic substitution. Zhang L, Qiu BY, Li X, Wang X, Li JY, Zhang YL, Liu J, Li J, Shen JK. Molecules 2006, 11:988-999. (IF: 0.841)
Construction of a small peptide library related to inhibitor OM99-2 and its structure-activity relationship to beta-secretase. Hu B, Xiong B, Qiu BY, Li X, Yu HP, Xiao K, Wang X, Li J, Shen JK. Acta Pharmacol Sin 2006, 27:1586-1593. (IF: 1.397)
Berberine-stimulated glucose uptake in L6 myotubes involves both AMPK and p38 MAPK. Cheng Z, Pang T, Gu M, Gao AH, Xie CM, Li JY, Nan FJ, Li J*. Biochim. Biophys. Acta 2006, 1760:1682-1689. (IF: 2.024)
Isoquinoline-1,3,4-trione and its derivatives attenuate b-amyloid-induced apoptosis of neuronal cells. Zhanga YH, Zhang HJ, Wu F, Chen YH, Ma XQ, Du JQ, Zhou ZL, Li JY, Nan FJ*, Li J*. FEBS J. 2006, 273:4842-4852. (IF:3.033)
Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B enhancing insulin receptor phosphorylation and stimulating glucose uptake. Zhang W, Hong D, Zhou YY, Zhang YN, Shen Q, Li JY, Hu LH*, Li J*. Biochim. Biophys. Acta 2006, 1760:1505-1512. (IF: 2.024)
Deturametelins H, I, and J: Three New Withanolide Glycosides from Datura metel L. Ma L, Xie CM, Li J, Lou FC, Hu LH. Chem. Biodivers. 2006, 3:180-186. (IF: 1.616)
Design and Synthesis of a Biotin-Tagged Photoaffinity Probe of Paeoniflorin. Qiu WW, Xu J, Liu DZ, Li JY, Ye Y, Zhu XZ, Li J*, Nan FJ*. Bioorg. Med. Chem. Lett. 2006, 16:3306-3309. (IF: 2.538)
Design, Synthesis and Evaluation of Leu*Ala Hydroxyethylene based Non-Peptide β-secretase (BACE) Inhibitors. Xiao K, Li X, Li JY, Ma LP, Hu B, Yu HP, Fu Y, Wang R*, Ma ZQ, Qiu BY, Li J*, Hu DY, Wang X, Shen JK*.Bioorg. Med. Chem. 2006, 14:4535-4551. (IF: 2.624)
Design, synthesis and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors. Chen YH, Zhang YH, Zhang HJ, Liu DZ, Gu M, Li JY, Wu F, Zhu XZ*, Li J*, Nan, , , FJ*. J. Med. Chem. 2006, 49:1613-1623. (IF:5.115)
Synthesis of mitirone analogues as inhibitors of Cdc25 phosphatases. Huang WG, Li JY, Zhang W, Zhou YY, Xie CM, Luo Y, Li YF, Wang JL, Li J*, Lu W*. Bioorg. Med. Chem. Lett. 2006, 16:1905-1908. (IF: 2.538)
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids. Ma DW, Jiang YW, Chen FP, Gong LK, Ding K, Xu Y, Wang RX, Ge AH, Ren J, Li JY, Li J, Ye QZ. J. Med. Chem. 2006, 49:456-458. (IF:5.115)
PTP1B inhibitors from Saussrurea Lappa. Li S, An TY, Li J, Shen Q, Lou FC, Hu LH. J Asian Nat Prod Res. 2006, 8:281-286. (IF: 0.828)
O-methyl nakafuran-8 lactone, a new sesquiterpenoid from a hainan marine sponge Dysidea sp. Shao ZY, Li J, Sim CJ, Li JY, Li ZY, Nan FJ, Guo YW. J Asian Nat Prod Res. 2006, 8:223-227. (IF: 0.828)
Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase. Yang XN, Li JY, Zhou YY; Shen Q, Chen JW, Li J*. Biochim. Biophys. Acta 2005, 1726:34-41. (IF: 2.024)
Identification of Potent Type I MetAPs Inhibitors by Simple Bioisosteric Replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives. Cui YM, Huang QQ, Xu J, Chen LL, Li JY, Ye QZ, Li J*, Nan FJ*. Bioorg. Med. Chem. Lett. 2005, 15:4130-4135. (IF: 2.538)
Identification of Potent Type I MetAPs Inhibitors by Simple Bioisosteric Replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT) derivatives. Cui YM, Huang QQ, Xu J, Chen LL, Li JY, Ye QZ, Li J*, Nan FJ*. Bioorg. Med. Chem. Lett. 2005, 15:3732-3736. (IF: 2.538)
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor a and their bioactivities in vivo. Yang CH, Xu GY, Li J, Wu XH, Liu B, Yan XM, Wang MW, Xie YY. Bioorg. Med. Chem. Lett. 2005, 15:1505-1507. (IF: 2.538)
PTP1B inhibitors from Ardisia japonica. Li YF, Hu LH, Lou FC, Li J, Shen Q. J Asian Nat Prod Res. 2005, 7:13-18. (IF: 0.828)
Furostanoside from Asparagus filicinus. Li YF, Hu LH, Lou FC, Hong JR, Li J, Shen Q. J Asian Nat Prod Res. 2005, 7:43-47. (IF: 0.828)
Synthesis and biological evaluation of (G)-cryptotanshinone and its simplified analogues as potent CDC25 inhibitors. Huang WG, Jiang YY, Li Q, Li J*, Li JY, Lu W*, Cai JC. Tetrahedron 2005, 61:1863-1870. (IF: 2.817)
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent. Luo Q, Li JY, Chen LL, Li J, Ye QZ, Nan FJ. Bioorg. Med. Chem. Lett. 2005, 13:639-644. (IF: 2.538)
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold. Luo Q, Li JY, Liu Z, Chen LL, Li J, Ye QZ, Nan FJ. Bioorg. Med. Chem. Lett. 2005, 13:635-638. (IF: 2.538)
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