100706-药理学

肿瘤药理学

2001-09--2004-07   郑州大学   博士

   

2013-09~现在, 中国科学院上海药物研究所, 研究员，课题组长
2011-01~2012-06,美国Hormel研究所, 博士后
2006-08~2013-08,中国科学院上海药物研究所, 副研究员
2004-08~2006-07,中国科学院上海药物研究所, 博士后
2001-09~2004-07,郑州大学, 博士
1994-08~2004-08,郑州大学, 助教，讲师

肿瘤药理学概论
肿瘤药理学
肿瘤药理

   

（1） 上海市五一劳动奖章, 市地级, 2021
（2） 抗肿瘤1类新药EGFR三代抑制剂ASK120067项目, 一等奖, 市地级, 2021

（ 1 ） 联苯甲酰胺类化合物及其应用, 2023, 第 2 作者, 专利号: 2023104812661

（ 2 ） 一类四氢苯并呋喃[2,3-c]吡啶类激酶抑制剂及其制备方法及用途, 2022, 第 4 作者, 专利号: 202211167412.5

（ 3 ） CSF1R激酶抑制剂及其用途, 2022, 第 3 作者, 专利号: CN114246864A

（ 4 ） 一种布鲁顿酪氨酸激酶抑制剂的用途, 2021, 第 4 作者, 专利号: CN202111235137.1

（ 5 ） 一类作为TBK1抑制剂的化合物、包含其的药物组合物及其用途, 2021, 第 4 作者, 专利号: 202110280860.5

（ 6 ） 一类IRAK4激酶抑制剂及其制备和应用, 2021, 第 4 作者, 专利号: CN112480101A

（ 7 ） 吲哚-1-碳酸酯类化合物、其制备方法和应用, 2021, 第 7 作者, 专利号: CN108250187B

（ 8 ） 一种2-氨基嘧啶类化合物的多晶型形式, 2020, 第 4 作者, 专利号: CN107417626B

（ 9 ） 一种2-氨基嘧啶类化合物的药用组合物及其制备方法, 2019, 第 6 作者, 专利号: CN110446701A

   

（1） A novel strategy for treating oncogene-mutant tumors by targeting tumor microenvironment and synergistically enhancing anti-PD1 immunotherapy, Cancer Communications, 2024, 
（2） From bench to bedside: current development and emerging trend of KRAS-targeted therapy, Acta Pharmacologica Sinica, 2024, 
（3） A Novel IRAK4 Inhibitor DW18134 Ameliorates Peritonitis and Inflammatory Bowel Disease, Molecules, 2024, 
（4） Discovery of a novel BTK inhibitor S-016 and identification of a new strategy for the treatment of lymphomas including BTK inhibitor-resistant lymphoma, Acta Pharmacologica Sinica, 2024, 
（5） Design, synthesis and pharmacological evaluation of 2,3-dihydrobenzofuran IRAK4 inhibitors for the treatment of diffuse large B-cell lymphoma, European Journal of Medicinal Chemistry, 2023, 
（6） Design and Synthesis of 1H-Pyrazolo[3,4-d]pyrimidine Derivatives as Hematopoietic Progenitor Kinase 1 (HPK1) inhibitors, Bioorganic Chemistry, 2023, 
（7） Discovery of HCD3514 as a potent EGFR inhibitor against C797S mutation in vitro and in vivo, JOURNAL OF CANCER, 2023, 第 19 作者  通讯作者
（8） Application of deep generative model for design of Pyrrolo2,3-d pyrimidine derivatives as new selective TANK binding kinase 1 (TBK1) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 7 作者  通讯作者
（9） Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 10 作者
（10） Design, synthesis and evaluation of (R)-8-((tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as novel selective ACK1 inhibitors to combat acquired resistance to the 3rd-generation EGFR inhibitor, JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 8 作者  通讯作者
（11） Design, synthesis and biological evaluation of KRASG12C-PROTACs as protein degraders, Bioorganic & Medicinal Chemistry, 2023, 第 9 作者  通讯作者
（12） 18F-Labeled o���aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging, BIOORGANIC & MEDICINAL CHEMISTRY, 2023, 第 7 作者  通讯作者
（13） Preclinical and early clinical studies of a novel compound SYHA1813 that efficiently crosses the blood-brain barrier and exhibits potent activity against GBM, Acta Pharma Sin B, 2023, 
（14） ASK120067 potently suppresses B-cell or T-cell malignancy in vitro and in vivo by inhibiting BTK and ITK, Frontiers in Pharmacology, 2022, 
（15） LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo, CANCER SCIENCE, 2022, 第 22 作者  通讯作者
（16） Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-GenerationEpidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 10 作者  通讯作者
（17） Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR(T790M/C797S) Mutants, ACS MEDICINAL CHEMISTRY LETTERS, 2022, 第 13 作者  通讯作者
（18） Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 11 作者  通讯作者
（19） Identification of 1H-pyrazolo3,4-bpyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2022, 第 8 作者  通讯作者
（20） ASK120067 (limertinib) Exerts Pre-clinical Anti-tumor Activity by Inhibiting EGFR Exon20 Insertion, Frontiers in Drug Discovery, 2022, 
（21） Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs, ACS Med Chem Lett, 2021, 
（22） Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors, Bioorganic & Medicinal Chemistry, 2021, 
（23） TANK-binding kinase 1 (TBK1): An emerging therapeutic target for drug discovery, DRUG DISCOVERY TODAY, 2021, 第 6 作者  通讯作者
（24） Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRASG12C inhibitors, European Journal of Medicinal Chemistry, 2021, 
（25） Discovery and biological evaluation of N-(3-(7-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-4-methyl-2-oxo-2Hpyrimido[4,5-d][1,3]oxazin-1(4H)-ly)phenyl)acrylamide as potent Bruton���s tyrosine kinase inhibitors, Acta Pharmacologica Sinica, 2020, 
（26） Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders, Journal of Medicinal Chemistry, 2020, 
（27） Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88L265P diffuse large B-cell lymphoma, European Journal of Medicinal Chemistry, 2020, 
（28） 2-Oxo-3,4-dihydropyrimido4,5-d pyrimidines as new reversible inhibitors of EGFR C797S(Cys797 to Ser797)mutant, 2-Oxo-3,4-dihydropyrimido4,5-d pyrimidines as new reversible inhibitors of EGFR C797S (Cys797 to Ser797) mutant, CHINESE CHEMICAL LETTERS, 2020, 第 10 作者  通讯作者
（29） Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance, MOLECULAR CANCER, 2020, 第 21 作者  通讯作者
（30） Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation, Bioorganic & Medicinal Chemistry Letters, 2020, 
（31） Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro, Chemical Papers, 2019, 
（32） Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR(L858R/T790M/C797S)), Journal of Medicinal Chemistry, 2019, 
（33） Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton���s tyrosine kinase inhibitors, Bioorganic & Medicinal Chemistry, 2019, 
（34） Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S, ACS Medicinal Chemistry Letters, 2019, 
（35） C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis, Acta Pharmacologica Sinica, 2019, 
（36） DW10075, a novel highly selective inhibitor of vascular endothelial growth factor receptor, exhibits antitumor activities both in vitro and in vivo., Acta Pharmacol Sin, 2016, 第 1 作者  通讯作者
（37） Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation, CHEMICAL BIOLOGY & DRUG DESIGN, 2016, 第 12 作者  通讯作者
（38） Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 第 13 作者  通讯作者
（39） Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 第 8 作者  通讯作者
（40） Design, synthesis and biological evaluation of biphenylurea derivatives as VEGFR-2 kinase inhibitors (II), CHINESE CHEMICAL LETTERS, 2016, 第 8 作者
（41） A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties., Eur J Med Chem, 2016, 第 1 作者  通讯作者
（42） C-5 Substituted Pyrido[2,3-d] pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinica resistance-related EGFRT790M mutant, MedChemComm, 2015, 第 1 作者  通讯作者
（43） Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I), CHINESE CHEMICAL LETTERS, 2015, 第 6 作者
（44） Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors, MEDCHEMCOMM, 2015, 第 7 作者  通讯作者
（45） 2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M), BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 第 13 作者  通讯作者
（46） Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors, ACS MEDICINAL CHEMISTRY LETTERS, 2014, 第 8 作者  通讯作者
（47） Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno2,3-dpyrimidines as irreversible epidermal growth factor receptor inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 第 10 作者  通讯作者
（48） Novel metal complexes of naphthalimide���cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 第 7 作者
（49） Topoisomerase II inhibitors from the roots of Stellera chamaejasme L., BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 第 7 作者  通讯作者
（50） Identification of DW532 as a novel anti-tumor agent targeting both kinase and tubulin, Acta Pharmacologica Sinica, 2014, 第 1 作者  通讯作者
（51） Naphthalimides exhibit invitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs), EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 第 9 作者
（52） Identification of an Aurora Kinase Inhibitor Specific for the Aurora B Isoform, CANCER RESEARCH, 2013, 第 1 作者
（53） Design, Synthesis and Biological Evaluation of novel 4-Anilinoquinazolines with C-6 Urea-linked side chains as the Epidermal Growth Factor Receptor (EGFR) Inhibitors, Bioorg Med Chem, 2013, 第 1 作者  通讯作者
（54） Discovery of the novel mTOR inhibitor and its antitumor activities in vitro and in vivo, MOLECULAR CANCER THERAPEUTICS, 2013, 第 1 作者
（55） Discovery of novel selective inhibitors for EGFR-T790M/L858R, BIOORGANICMEDICINALCHEMISTRYLETTERS, 2012, 第 10 作者
（56） Identification of mammalian target of rapamycin (mTOR) as a direct target of fenretinib both in vitro and in vivo., Carcinogenesis, 2012, 第 1 作者
（57） Novel Acenaphtho[1,2-b]pyrrole Derivatives as Potent and Selective Fibroblast Growth Factor Receptors 1 Inhibitors: Design, Synthesis and Biological Evaluation., Journal of Medicinal Chemistry, 2011, 第 1 作者  通讯作者
（58） AST1306, an irreversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, exhibits its anticancer activities both in vitro and in vivo., 2011, 第 1 作者
（59） Establishment of platform for screening insulin-like growth factor-1 receptor inhibitors and evaluation of novel inhibitors, Establishment of platform for screening insulin-like growth factor-1 receptor inhibitors and evaluation of novel inhibitors, 中国药理学报：英文版, 2011, 第 2 作者
（60） Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening, JOURNAL OF MEDICINAL CHEMISTRY, 2010, 第 2 作者  通讯作者

（ 1 ） 《高等药理学》（第二版）, 科学出版社, 2019-07, 第 其他 作者
（ 2 ） 个性化药物：新药研发的未来, 上海科学技术文献出版社, 2020-03, 第 其他 作者
（ 3 ） 大肠癌：基础与临床的转化, 上海交通大学出版社, 2020-06, 第 其他 作者

   

（ 1 ） 候选新药耐药机制和肿瘤免疫新靶标探索, 负责人, 研究所自主部署, 2023-10--2026-09
（ 2 ） BCAT1作为肿瘤耐药关键靶标的确证及克服BCAT1介导耐药的候选药物发现, 参与, 中国科学院计划, 2023-01--2024-12
（ 3 ） 支链氨基酸转氨酶1（BCAT1）介导EGFR三代抑制剂耐药机制研究, 负责人, 国家任务, 2023-01--2026-12
（ 4 ） 克服肺癌耐药新型抑制剂研发, 负责人, 中国科学院计划, 2022-06--2025-06
（ 5 ） 三阴性乳腺癌转移的分子机制研究, 参与, 中国科学院计划, 2022-06--2025-06
（ 6 ） 肺癌耐药新靶标的发现与确证及抑制剂研究, 负责人, 中国科学院计划, 2022-05--2023-05
（ 7 ） EGFR T790M耐药突变选择性抑制剂120067生物标志物研究, 负责人, 中国科学院计划, 2016-05--2018-12
（ 8 ） 新型VEGFR抑制剂抗肿瘤作用及生物标志物研究, 负责人, 中国科学院计划, 2015-09--2016-09

（1）分子靶向抗肿瘤药物研发及标志物研究   河南省药理学会肿瘤药理专业委员会2022年学术年会   2022-12-31
（2）新型EGFR三代抑制剂ASK120067抗肿瘤作用及标志物研究   四届东方药理论坛上海市药理学会第二十二届学术年会   2021-12-16
（3）Identification of novel inhibitors against EGFR T790M resistance mutation   2016-12-07