基本信息
李静雅  女  博导  中国科学院上海药物研究所
电子邮件: jyli@mail.shcnc.ac.cn
通信地址: 上海市张江高科技园区郭守敬路189号
邮政编码: 201203

招生信息

   
招生专业
100706-药理学
招生方向
代谢性疾病药理学

教育背景

1998-09--2003-07   中科院上海药物研究所   博士学位
1994-09--1998-07   华东师范大学   学士学位
1991-09--1994-07   浙江省温州中学   高中

工作经历

   
工作简历
2009-09~现在, 中国科学院上海药物研究所, 博士研究生导师
2008-08~现在, 中科院上海药物研究所, 研究员
2006-07~2009-08,中国科学院上海药物研究所, 硕士研究生导师
2005-07~2008-07,中科院上海药物研究所, 副研究员
2003-07~2005-07,中科院上海药物研究所, 助理研究员
1998-09~2003-07,中科院上海药物研究所, 博士学位
1994-09~1998-07,华东师范大学, 学士学位
1991-09~1994-07,浙江省温州中学, 高中

专利与奖励

   
奖励信息
(1) 2. 2015上海市浦东新区科技进步一等奖, 一等奖, 市地级, 2015
(2) 1. 2004年中国药理学会施维雅青年科学工作者奖, 专项, 2004
专利成果
( 1 ) 一类4-羟基戊酰胺类化合物及其制备方法和用途, 2005, 第 4 作者, 专利号: ZL200510023951.1
( 2 ) 一类杂环衍生物、制备方法及其用途, 2003, 第 5 作者, 专利号: ZL03142277.2
( 3 ) 一类喹喔啉类衍生物、制法及用途, 2005, 第 4 作者, 专利号: ZL200510110483.1
( 4 ) 一类4-羟基戊酰胺类化合物及其制备方法和用途, 2005, 第 4 作者, 专利号: ZL200510023951.1
( 5 ) 一种新型抗糖尿病化合物及其制备方法和用途, 2010, 第 4 作者, 专利号: CN2010101046339
( 6 ) 联苯化合物及其制备方法和用途, 2009, 第 5 作者, 专利号: CN200910044875.0
( 7 ) 蛋白酪氨酸磷酸酯酶1B抑制剂及其制备方法和用途, 2008, 第 5 作者, 专利号: PCT/CN2008/00400
( 8 ) 蛋白酪氨酸磷酸酯酶1B抑制剂及其制备方法和用途, 2007, 第 5 作者, 专利号: CN200710037848.1
( 9 ) 13, 13a-二氢小檗碱衍生物及其药物组合物和用途, 2006, 第 5 作者, 专利号: CN200610140429.6
( 10 ) 4-羟基戊酰胺类化合物及其制备方法和用途, 2006, 第 5 作者, 专利号: PCT/CN2006/000035
( 11 ) 一类喹喔啉类衍生物、制法及用途, 2005, 第 4 作者, 专利号: CN200510110483.1
( 12 ) 一类小分子探针设计的结构模块、制备方法及用途, 2005, 第 3 作者, 专利号: CN200510028485.6
( 13 ) 一类4-羟基戊酰胺类化合物及其制备方法和用途, 2005, 第 4 作者, 专利号: CN200510023951.1
( 14 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2018, 第 4 作者, 专利号: CA2857537A1
( 15 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2016, 第 4 作者, 专利号: 5968455
( 16 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2016, 第 4 作者, 专利号: KR101718596B1
( 17 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2016, 第 4 作者, 专利号: RU2624021
( 18 ) 一类螺异噁唑啉衍生物、其制备方法及医药用途, 2016, 第 4 作者, 专利号: ZL 2014101122063
( 19 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2016, 第 4 作者, 专利号: ZL201210262331.3
( 20 ) 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途, 2016, 第 4 作者, 专利号: US009045491B2
( 21 ) 一种可用作人源腺苷单核苷酸激活蛋白激酶激活剂的化合物及其制备方法和应用, 2010, 第 5 作者, 专利号: ZL2006/002685
( 22 ) 13, 13α-二氢小檗碱衍生物及其药物组合物和用途, 2009, 第 5 作者, 专利号: ZL200610140429.6
( 23 ) 13, 13α-二氢小檗碱衍生物及其药物组合物和用途, 2009, 第 5 作者, 专利号: 2070926
( 24 ) 蛋白酪氨酸磷酸酯酶1B抑制剂及其制备方法和用途, 2012, 第 5 作者, 专利号: US 8,183,383 B2
( 25 ) 蛋白酪氨酸磷酸酯酶1B抑制剂及其制备方法和用途, 2012, 第 5 作者, 专利号: ZL200710037848.1
( 26 ) 8,8-二取代-13,13a-二氢小檗碱衍生物及其药物组合物和用途, 2009, 第 4 作者, 专利号: ZL200910049688.1

出版信息

   
发表论文
(1) Structural Elucidation and Bio-inspired Total Synthese of Ascorbylated Diterpenoid Hongkonoids A-D, J Am Chem Soc, 2018, 第 8 作者
(2) AMP-activated protein kinase(AMPK) regulates energy metabolism through modulating thermogenesis in adipose tissue, FRONT PHYSIOL, 2018, 通讯作者
(3) Novel Substituted Pyrazolone Derivatives as AMP-Activated Protein Kinase Activators to Inhibit Lipid Synthesis and Reduce Lipid Accumulation in ob/ob Mice, Acta PHARMACOLOGICA SINICA, 2018, 通讯作者
(4) Discovery of Benzofuran-3(2H)-one Derivatives as Novel DRAK2 Inhibitors that Protect Islet beta-cells from Apoptosis, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 通讯作者
(5) The Landscape of Histone Modifications in a High-Fat Diet-Induced Obese (DIO) Mouse Model, MOLECULAR & CELLULAR PROTEOMICS, 2017, 通讯作者
(6) Isoprenylated Phenolic Compounds with PTP1B Inhibition from Morus Alba, FITOTERAPIA, 2017, 第 4 作者
(7) Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(8) Metabolic Regulation of Gene Expression by Histone Lysine beta-Hydroxybutyrylation, MOLECULAR CELL, 2016, 第 8 作者
(9) Design,synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity, Bioorganic & Medicinal Chemistry Letters, 2016, 第 4 作者
(10) 2-(3-Benzoylthioureido)-4,5,6,7-tetrahydrobenzo[b] thiophene-3-carboxylic acid ameliorates metabolic disorders in high-fat diet-fed mice, Acta Pharmacologica Sinica, 2015, 通讯作者
(11) Synthesis and biological evaluation of novel 2,3-pyrazole ring-substituted-4,4-dimethyl lithocholic acid derivatives as selective protein tyrosine phosphatase 1B (PTP1B) inhibitors with cellular efficacy, RSC Advances, 2015, 通讯作者
(12) Isoprenylated Flavonoids with PTP1B Inhibition from Ficus tikoua, Natural Product Communications, 2015, 第 4 作者
(13) Hydroxylated Daphniphyllum Alkaloids from Daphniphyllum himalense, Journal of Natural Products, 2015, 第 4 作者
(14) Synthesis of Novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene Derivatives and Their Biological Evaluation Against Protein Tyrosine Phosphatase 1B, Chemical Biology & Drug Design, 2015, 第 4 作者
(15) Two Enantiomeric Pairs of Meroterpenoids from Rhododendron capitatum, Organic Letters, 2015, 第 4 作者
(16) New Isoprenylated Phenolic Compounds from Morus laevigata, Chemistry and Biodiversity, 2015, 第 4 作者
(17) Design andsynthesis of novel 1,2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors, Bioorganic & Medicinal Chemistry Letters, 2015, 第 4 作者
(18) PTP1B inhibitors from stems of Angelica keiskei (Ashitaba), Bioorganic & Medicinal Chemistry Letters, 2015, 第 4 作者
(19) Diels-Alder adducts with PTP1B inhibition from Morus notabilis, Phytochemistry, 2015, 第 4 作者
(20) Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles, European Journal of Medicinal Chemistry, 2014, 通讯作者
(21) Azoxystrobin, a mitochondrial complex III Q(o) site inhibitor, exerts beneficial metabolic effects in vivo and in vitro, Biochimicaet Biophysica Acta-General Subjects, 2014, 通讯作者
(22) Lihong(*),Discovery, synthesis, and structure activity relationships of 20(S)-protopanaxadiol (PPD) derivatives as a novel class of AMPK alpha 2 beta 1 gamma 1 activators, European Journal of Medicinal Chemistry, 2014, 通讯作者
(23) Discovery of a novel inhibitor of NAD(P)(+)-dependent malic enzyme (ME2) by high-throughput screening, Acta Pharmacologica Sinica, 2014, 通讯作者
(24) (R)-3-Amino-1-((3aS,7aS)-octahydro-1H-indol-1 -yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: Design, synthesis, biological evaluation, and molecular modeling, Bioorganic & Medicinal Chemistry, 2014, 第 4 作者
(25) Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors, European Journal of Medicinal Chemistry, 2014, 第 4 作者
(26) Novel grayanane diterpenoids from Rhododendron principis, Tetrahedron, 2014, 第 4 作者
(27) 8,8-Dimethyldihydroberberine with improved bioavailability and oral efficacy on obese and diabetic mouse models., Bioorg. Med. Chem. , 2010, 通讯作者
(28) Phenolic compounds from the leaves of Cyclocarya paliurus (Batal.) Ijinskaja and their inhibitory activity against PTP1B., Food Chem. , 2010, 第 4 作者
(29) A high-throughput assay for modulators of mitochondrial membrane potential identifies a novel compound with beneficial effects on db/db mice., Diabetes, 2010, 通讯作者
(30) 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., Diabetes, 2008, 第 1 作者
(31) Corosolic acid stimulates glucose uptake via enhancing insulin receptor phosphorylation., Eur. J Pharmacol., 2008, 通讯作者
(32) Activity-based protein profiling for type I methionine aminopeptidase by the use of photo-affinity tri-modular probes., Chem. Bio. Chem., 2007, 第 1 作者
(33) Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors.,  Bioorg. Med. Chem. Lett. , 2007, 通讯作者
(34) Conserved alpha helix act as autoinhibitory sequence in AMP-activated protein kinase alpha subunits., J Biol. Chem. , 2007, 第 3 作者
(35) Preparation of 6-substituted quinoxaline JSP-1 inhibitors by microwave accelerated nucleophilic substitution. , Molecules, 2007, 通讯作者
(36) Design and Synthesis of a Biotin-Tagged Photoaffinity Probe of Paeoniflorin. , Bioorg. Med. Chem. Lett. , 2006, 第 4 作者
(37) Design, Synthesis and Evaluation of Leu*Ala Hydroxyethylene based Non-Peptide β-secretase (BACE) Inhibitors., Bioorg. Med. Chem. , 2006, 第 3 作者
(38) O-methyl nakafuran-8 lactone, a new sesquiterpenoid from a hainan marine sponge Dysidea sp., J Asian Nat Prod Res. , 2006, 第 4 作者
(39) Synthesis of Mitirone Analogues as Inhibitors of Cdc25 Phosphatases., Bioorg. Med. Chem. Lett. , 2005, 第 2 作者
(40) Discovery of novel inhibitor of human leukocyte common antigen-related phosphatase.,  Biochim. Biophys. Acta , 2005, 第 2 作者
(41) Identification of Potent Type I MetAPs Inhibitors by Simple Bioisosteric Replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives. , Bioorg. Med. Chem. Lett. , 2005, 通讯作者
(42) 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. , Bioorg. Med. Chem. Lett., 2005, 通讯作者
(43) Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold., Bioorg. Med. Chem. Lett., 2005, 第 2 作者
(44) Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent. , Bioorg. Med. Chem. Lett. , 2005, 第 2 作者
(45) Synthesis and biological evaluation of (G)-cryptotanshinone and its simplified analogues as potent CDC25 inhibitors., Tetrahedron , 2005, 通讯作者
(46) Mutations at the S1 site of methionine aminopeptidases from Escherichia coli and Homo sapiens reveal the residues critical for substrate specificity. , J. Biol. Chem. , 2004, 第 1 作者
(47) Characterization of full length and truncated type I human methionine aminopeptidase expressed from Escherichia coli., Biochemistry , 2004, 第 1 作者
(48) Design and Synthesis of Chromogenic Thiopeptolide Substrates as MetAPs Active Site Probes., Bioorg. Med. Chem., 2004, 第 2 作者
(49) Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening., Acta. Pharmacologica. Sinica., 2004, 第 3 作者
(50) Tetrahydroisoquinoline base sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors., Bioorg. Med. Chem. Lett. , 2004, 第 4 作者
(51) Metal substitution of Methionine Aminopeptidases from Escherichia coli Changes Specificity for Substrates and Inhibitors. , Biochem. Biophys. Res. Commun., 2003, 第 1 作者
(52) Discovery and Structural Modification of Inhibitors of Methionine Aminopeptidases from Escherichia coli and Saccharomyces cereviaiae., J. Med. Chem. , 2003, 第 2 作者

科研活动

   
科研项目
( 1 ) 靶向DPP-4的超长效降糖候选药物研究, 主持, 部委级, 2015-09--2016-08
( 2 ) 2型糖尿病肾病药物新靶标和候选药物的临床前研究, 主持, 国家级, 2016-09--2020-12
( 3 ) 双靶向“线粒体偶联效率和丙酮酸脱氢酶复合物PDC活性”策略改善高血糖症, 主持, 国家级, 2017-01--2020-12
( 4 ) 抗糖尿病候选药物DC892081的临床前研究, 主持, 部委级, 2016-08--2018-08
( 5 ) 新颖线粒体功能调节改善2型糖尿病, 主持, 省级, 2016-07--2019-06
( 6 ) AMPK小分子激活剂YLF466D的抗糖尿病药理作用机制研究, 主持, 国家级, 2013-01--2016-12
( 7 ) 小檗碱促进白色脂肪米色化的药理活性评价及作用机制研究, 主持, 国家级, 2015-01--2016-12
( 8 ) 靶向一磷酸腺苷激活蛋白激酶AMPK的抗糖尿病候选药物的筛选研究, 主持, 省级, 2014-07--2017-09
( 9 ) 药物发现前沿关键技术的研究、优化与应用, 主持, 国家级, 2013-01--2015-12