100706-药理学

抗肿瘤药物药理

1996-09--2001-07   中科院上海药物研究所   理学博士
1992-09--1996-09   华东师范大学   理学学士

   

2006-03~现在, 中科院上海药物研究所, 副研究员，研究员
2001-09~2006-03,美国国立癌症研究所, 博士后
1996-09~2001-07,中科院上海药物研究所, 理学博士
1992-09~1996-09,华东师范大学, 理学学士

2023-03-01-2026-02-28,上海市抗癌协会, 理事
2022-12-01-2026-11-30,上海市药理学会, 理事
2012-12-01-今,Acta Pharmacologica Sinica 编委, 编委
2007-07-01-今,中国抗癌协会抗癌药物专业委员会, 第四届委员会委员
2007-07-01-今,中国药理学会肿瘤药理专业委员会, 委员

   

（ 1 ） 含杂环侧链的噁二唑衍生物、合成方法及其应用, 2019, 第 2 作者, 专利号: CN110143955A

（ 2 ） 7-位取代吡咯并三嗪类化合物或其药学上可用的盐，及其制备方法和用途, 2019, 第 2 作者, 专利号: CN109111447A

（ 3 ） 去氮嘌呤类化合物及其药物组合物、制备方法和用途, 2018, 第 2 作者, 专利号: CN107722013A

（ 4 ） 蛋白激酶抑制剂, 2017, 第 3 作者, 专利号: CN107207441A

（ 5 ） 一类取代喹唑啉-4-酮类化合物及其制备方法和医药用途, 2017, 第 2 作者, 专利号: CN106995438A

（ 6 ） 双环稠杂环化合物及其用途和药物组合物, 2014, 第 3 作者, 专利号: CN103626783A

（ 7 ） 一类吡唑并吡啶类化合物及其制备方法、用途和药物组合物, 2014, 第 3 作者, 专利号: CN103570709A

（ 8 ） 吡咯2,1-f1,2,4并三嗪类化合物,其制备方法及用途, 2013, 第 2 作者, 专利号: CN103450204A

（ 9 ） 一类三嗪类化合物、该化合物的制备方法及其用途, 2013, 第 4 作者, 专利号: CN102887867A

（ 10 ） 一类噻唑类化合物及其制备方法和用途, 2012, 第 8 作者, 专利号: CN102775368A

（ 11 ） 一种检测化合物对人Ⅰ型PI3Ks抑制活性的方法, 2012, 第 1 作者, 专利号: CN102719517A

（ 12 ） 一类吲唑类化合物及其制备方法、用途和药物组合物, 2012, 第 2 作者, 专利号: CN102675286A

（ 13 ） 一种对映-贝壳杉烷型二萜及其衍生物和制备方法, 2012, 第 5 作者, 专利号: CN102584760A

（ 14 ） 吡啶并吡咯三嗪化合物、其制备方法和用途, 2012, 第 2 作者, 专利号: CN102558185A

（ 15 ） 菲并吲哚里西啶生物碱衍生物及其盐和抗癌活性, 2011, 第 2 作者, 专利号: CN102002041A

（ 16 ） 一类新型苯并蒽环类化合物及其制备方法和用途, 2011, 第 2 作者, 专利号: CN101993446A

（ 17 ） 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途, 2010, 第 5 作者, 专利号: CN101676291A

   

（1） Adaptive resistance to PI3K alpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells, CELL DEATH & DISEASE, 2021, 通讯作者
（2） PI3K alpha inhibitor impairs AKT phosphorylation and synergizes with novel angiogenesis inhibitor AL3810 in human hepatocellular carcinoma, SIGNAL TRANSDUCTION AND TARGETED THERAPY, 2021, 第 5 作者
（3） SAF-248, a novel PI3K delta-selective inhibitor, potently suppresses the growth of diffuse large B-cell lymphoma, ACTA PHARMACOLOGICA SINICA, 2021, 通讯作者
（4） 多靶点抗肿瘤天然产物研究进展, Research progress in multi-targeted anti-tumor natural products, 药学学报, 2021, 第 2 作者
（5） Corrigendum to "Systematic combination screening reveals synergism between rapamycin and sutent against human lung cancer" Cancer Letter 342(2014) 159-166, CANCER LETTERS, 2020, 第 4 作者
（6） 源于天然产物或其衍生物的分子靶向抗肿瘤药物研究进展, Progress in molecularly targeted anti-tumor drugs derived from natural products or their derivatives, 药学学报, 2020, 第 2 作者
（7） Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo2,1-f1,2,4triazine derivatives, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 通讯作者
（8） CRISPR-cas9: a powerful tool towards precision medicine in cancer treatment, crisprcas9apowerfultooltowardsprecisionmedicineincancertreatment, ACTA PHARMACOLOGICA SINICA, 2020, 通讯作者
（9） Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors., EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2020, 通讯作者
（10） Discovery and characterization of natural products as novel indoleamine 2,3-dioxygenase 1 inhibitors through high-throughput screening, Discovery and characterization of natural products as novel indoleamine 2,3-dioxygenase 1 inhibitors through high-throughput screening, ACTA PHARMACOLOGICA SINICA, 2020, 通讯作者
（11） Systematic combination screening reveals synergism between rapamycin and sutent against human lung cancer (vol 342, pg 159, 2014), CANCER LETTERS, 2020, 通讯作者
（12） Simultaneous inhibition of PI3K alpha and CDK4/6 synergistically suppresses Kras-mutated non-small cell lung cancer, MOLECULAR CANCER RESEARCH, 2020, 第 8 作者
（13） Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho -Naphthaquinone-Containing Natural Product, MOLECULES, 2019, 通讯作者
（14） Unbiased screening reveals that blocking exportin 1 overcomes resistance to PI3K alpha inhibition in breast cancer, SIGNAL TRANSDUCTION AND TARGETED THERAPY, 2019, 通讯作者
（15） Design, synthesis, and biological evaluation of thieno3,2-dpyrimidine derivatives as potential simplified phosphatidylinositol 3-kinase alpha inhibitors, CHEMICAL BIOLOGY & DRUG DESIGN, 2019, 通讯作者
（16） Design, synthesis, and biological activity evaluation of (-)-6-O-desmethylantofine analogues as potent anti-cancer agents, BIOORGANIC & MEDICINAL CHEMISTRY, 2019, 通讯作者
（17） Simultaneous inhibition of PI3K alpha and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer, CANCER BIOLOGY & MEDICINE, 2019, 通讯作者
（18） HRAS(G12s) mutant mediates resistance to a PI3K alpha inhibitor CYH33 in esophageal squamous cell carcinomas, MOLECULAR CANCER THERAPEUTICS, 2019, 第 9 作者
（19） Membrane metallo-endopeptidase mediates cellular senescence induced by oncogenic PIK3CA(H1047R) accompanied with pro-tumorigenic secretome, INTERNATIONAL JOURNAL OF CANCER, 2019, 通讯作者
（20） PI3K alpha inhibitors sensitize esophageal squamous cell carcinoma to radiation by abrogating survival signals in tumor cells and tumor microenvironment, CANCER LETTERS, 2019, 通讯作者
（21） Simultaneous inhibition of PI3Kα and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer, CANCER BIOLOGY AND MEDICINE, 2019, 其他（合作组作者）
（22） Simultaneous inhibition of PI3Kα and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer, simultaneousinhibitionofpi3kandcdk46synergisticallysuppresseskrasmutatednonsmallcelllungcancer, 癌症生物学与医学:英文版, 2019, 其他（合作组作者）
（23） Decrease in phosphorylated ERK indicates the therapeutic efficacy of a clinical PI3K alpha-selective inhibitor CYH33 in breast cancer, CANCER LETTERS, 2018, 通讯作者
（24） Discovery of clinical candidate methyl (5-(6-((4(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo2,1-f1,2,4triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) : A highly potent and selective PI3K alpha inhibitor for the treatment of advanced solid tumors, CANCER RESEARCH, 2018, 第 9 作者
（25） Oncogene-induced senescence: a double edged sword in cancer, ACTA PHARMACOLOGICA SINICA, 2018, 通讯作者
（26） The mTOR inhibitor AZD8055 overcomes tamoxifen resistance in breast cancer cells by down-regulating HSPB8, ACTA PHARMACOLOGICA SINICA, 2018, 通讯作者
（27） Oncogene-induced senescence: a double edged sword in cancer, Oncogene-induced senescence: a double edged sword in cancer, 中国药理学报：英文版, 2018, 第 3 作者
（28） Docking-based structural splicing and reassembly strategy to develop novel deazapurine derivatives as potent B-Raf V600E inhibitors, ACTA PHARMACOLOGICA SINICA, 2017, 通讯作者
（29） Integration of Receptor Tyrosine Kinases Determines Sensitivity to PI3K alpha-selective Inhibitors in Breast Cancer, THERANOSTICS, 2017, 通讯作者
（30） Discovery of a Novel Series of 7-AzaindoleScaffold Derivatives as PI3K Inhibitors with Potent Activity, ACS MEDICINAL CHEMISTRY LETTERS, 2017, 通讯作者
（31） 6-OH-Phenanthroquinolizidine Alkaloid and Its Derivatives Exert Potent Anticancer Activity by Delaying S Phase Progression, JOURNAL OF MEDICINAL CHEMISTRY, 2017, 通讯作者
（32） New Insights into PI3K Inhibitor Design using X-ray Structures of PI3K alpha Complexed with a Potent Lead Compound, SCIENTIFIC REPORTS, 2017, 通讯作者
（33） Targeting PI3K: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond, MEDICINAL RESEARCH REVIEWS, 2015, 第 6 作者
（34） Toward rapamycin analog (rapalog)-based precision cancer therapy, ACTA PHARMACOLOGICA SINICA, 2015, 第 1 作者
（35） PI3K isoform-selective inhibitors: next-generation targeted cancer therapies, ACTA PHARMACOLOGICA SINICA, 2015, 第 3 作者
（36） Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors, CHINESE CHEMICAL LETTERS, 2015, 通讯作者
（37） Identification of a Non-Gatekeeper Hotspot for Drug ResistantMutations in mTOR Kinase, CELL REPORTS, 2015, 第 4 作者
（38） Toward rapamycin analog (rapalog)-based precision cancer therapy, Toward rapamycin analog (rapalog)-based precision cancer therapy, 中国药理学报：英文版, 2015, 第 1 作者
（39） 新娃儿藤碱类似物抗肿瘤作用机制研究, 2015, 第 6 作者
（40） DW09849, a Selective Phosphatidylinositol 3-Kinase (PI3K) Inhibitor, Prevents PI3K Signaling and Preferentially Inhibits Proliferation of Cells Containing the Oncogenic Mutation p110 alpha (H1047R), JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2014, 通讯作者
（41） HSP90 inhibitor AUY922 abrogates up-regulation of RTKs by mTOR inhibitor AZD8055 and potentiates its antiproliferative activity in human breast cancer, INTERNATIONAL JOURNAL OF CANCER, 2014, 通讯作者
（42） Simultaneous targeting of PI3K delta and a PI3K delta-dependent MEK1/2-Erk1/2 pathway for therapy in pediatric B-cell acute lymphoblastic leukemia, ONCOTARGET, 2014, 通讯作者
（43） Systematic combination screening reveals synergism between rapamycin and sunitinib against human lung cancer, CANCER LETTERS, 2014, 第 4 作者
（44） Crystal Structures of PI3K alpha Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design, ACS MEDICINAL CHEMISTRY LETTERS, 2014, 通讯作者
（45） A pharmacological model reveals biased dependency on PI3K isoforms for tumor cell growth, ACTA PHARMACOLOGICA SINICA, 2013, 第 5 作者
（46） Different salt derivatives of phenanthroindolizidine alkaloids display different in vitro antitumor activity, NEW JOURNAL OF CHEMISTRY, 2013, 第 6 作者
（47） Inhibition of chemokine (CXC motif) ligand 12/chemokine (CXC motif) receptor 4 axis (CXCL12/CXCR4)-mediated cell migration by targeting mammalian target of rapamycin (mTOR) pathway in human gastric carcinoma cells., JOURNAL OF BIOLOGICAL CHEMISTRY, 2012, 第 6 作者
（48） Characterization of dihydroartemisinin-resistant colon carcinoma HCT116/R cell line, MOLECULAR AND CELLULAR BIOCHEMISTRY, 2012, 第 4 作者
（49） Inhibition of tumor cell growth, proliferation and migration by X-387, a novel active-site inhibitor of mTOR, BIOCHEMICAL PHARMACOLOGY, 2012, 第 6 作者
（50） Discovery and bioactivity of 4-(2-arylpyrido3′,2′:3,4pyrrolo1,2-f1,2,4triazin-4-yl) morpholine derivatives as novel PI3K inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 通讯作者
（51） Discovery and bioactivity of ylmorpholine derivatives as novel PI3K inhibitors., 2012, 通讯作者
（52） Inhibition of tumor cell growth, proliferation and migration by X-387, a novel active-site inhibitor of tumor., 2012, 通讯作者
（53） 土槿皮乙酸减弱非转录功能的c-Jun对缺氧诱导因子1α的稳定作用, 2011, 第 3 作者
（54） Total Synthesis of 7-Ethyl-10-hydroxycamptothecin (SN38) and its Application to the Development of C18-Functionalized Camptothecin Derivatives, CHEMISTRY-A EUROPEAN JOURNAL, 2011, 通讯作者
（55） 新型ATP竞争性mTOR抑制剂X-387抗肿瘤作用机制研究, 2011, 第 3 作者
（56） Characterization of dihydroartemisinin-resistant colon carcinoma HCT116/R cell line., MOLCELLBIOCHEM, 2011, 通讯作者
（57） PH006, a novel and selective Src kinase inhibitor, suppresses human breast cancer growth and metastasis in vitro and in vivo, BREAST CANCER RESEARCH AND TREATMENT, 2011, 通讯作者
（58） PI3K-δ选择性抑制剂X370对白血病细胞增殖抑制作用的研究, 2011, 第 3 作者
（59） The anti-cancer activity of dihydroartemisinin is associated with induction of iron-dependent endoplasmic reticulum stress in colorectal carcinoma HCT116 cells, INVESTIGATIONAL NEW DRUGS, 2011, 第 5 作者
（60） A Series of alpha-Heterocyclic Carboxaldehyde Thiosemicarbazones Inhibit Topoisomerase II alpha Catalytic Activity, JOURNAL OF MEDICINAL CHEMISTRY, 2010, 通讯作者
（61） Synthesis of N~(11)-anchoring biotinylated artemisinin derivatives and their preliminary biological assessment, SCIENCE CHINA-CHEMISTRY, 2010, 通讯作者
（62） WJD008, a Dual Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin Inhibitor, Prevents PI3K Signaling and Inhibits the Proliferation of Transformed Cells with Oncogenic PI3K Mutant, JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2010, 第 8 作者
（63） Dihydroartemisinin accelerates c-MYC oncoprotein degradation and induces apoptosis in c-MYC-overexpressing tumor cells, BIOCHEMICAL PHARMACOLOGY, 2010, 通讯作者
（64） Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase, BIOORGANIC & MEDICINAL CHEMISTRY, 2010, 通讯作者
（65） New microtubule-inhibiting anticancer agents, EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2010, 通讯作者
（66） 新型Src激酶抑制剂PH006的抗肿瘤作用研究, 2009, 第 3 作者
（67） S9, a novel anticancer agent, exerts its anti -proliferative activity by interfering with both PI3K-Akt-mTOR signaling and microtubule cytoskeleton, CANCER RESEARCH, 2009, 第11作者
（68） 二氢青蒿素促进癌蛋白c-MYC降解并诱发c-myc高表达的癌细胞凋亡, 2009, 第 2 作者
（69） Synthesis Study on Marmycin A: Preparation of the C3 '-Desmethyl Analogues, JOURNAL OF ORGANIC CHEMISTRY, 2009, 第 8 作者
（70） S9, a Novel Anticancer Agent, Exerts Its Anti-Proliferative Activity by Interfering with Both PI3K-Akt-mTOR Signaling and Microtubule Cytoskeleton, PLOS ONE, 2009, 第11作者
（71） Direct Palladium-Catalyzed Arylations of Aryl Bromides with 2/9-Substituted Pyrimido5,4-bindolizines, JOURNAL OF COMBINATORIAL CHEMISTRY, 2009, 第 3 作者
（72） Dihydroartemisinin accelerates c-Myc oncoprotein degradation and induces apoptosis in c-Myc overexpressed tumor cells, CANCER RESEARCH, 2009, 第 2 作者
（73） 缩氨基硫脲类新化合物TSC的抗肿瘤作用及其分子机制研究, 2009, 第 3 作者
（74） Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines, LETTERS IN ORGANIC CHEMISTRY, 2009, 第 4 作者
（75） 同时靶向PI3K/mTOR和微管的双重抑制剂的S9抗肿瘤作用, 2009, 第11作者
（76） Dihydroartemisinin induces apoptosis in HL-60 leukemia cells dependent of iron and p38 mitogen-activated protein kinase activation but independent of reactive oxygen species, CANCER BIOLOGY & THERAPY, 2008, 通讯作者
（77） ADAM15 suppresses cell motility by driving integrin alpha 5 beta 1 cell surface expression via Erk inactivation, INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY, 2008, 第 2 作者
（78） The Marine-Derived Oligosaccharide Sulfate (MdOS), a Novel Multiple Tyrosine Kinase Inhibitor, Combats Tumor Angiogenesis both In Vitro and In Vivo, PLOS ONE, 2008, 第 3 作者
（79） 双灵固本散对DNA拓扑异构酶的抑制作用及诱导K562细胞凋亡的研究, 浙江中医杂志, 2007, 第 3 作者
（80） RNA干扰技术的研究进展, Research progresses of RNA interference, 中国药理学通报, 2007, 第 2 作者
（81） Gambogic acid inhibits the catalytic activity of human topoisomerase II alpha by binding to its ATPase domain, MOLECULAR CANCER THERAPEUTICS, 2007, 第 2 作者
（82） Salvicine, a novel topoisomerase II inhibitor, exerts its potent anticancer activity by ROS generation1, ACTA PHARMACOLOGICA SINICA, 2007, 第 1 作者
（83） Salvicine, a novel topoisomerase II inhibitor, exerts its potent anticancer activity by ROS generation, ACTA PHARMACOLOGICA SINICA, 2007, 第 1 作者
（84） Emerging cancer therapeutic opportunities target DNA-repair systems, TRENDS IN PHARMACOLOGICAL SCIENCES, 2006, 第 3 作者
（85） 以DNA拓扑异构酶Ⅱ为靶点的抗癌药物, Anticancer drugs targeting DNA topoisomerase II, 中国新药杂志, 2002, 第 1 作者
（86） DNA拓扑异构酶Ⅱ是salvicine作用于酿酒酵母的主要靶点, 中国药理学报：英文版, 2001, 第 1 作者
（87） 鸦胆子油乳具有多药耐药逆转和拓扑异构酶Ⅱ抑制作用, 中国药理学通报, 2001, 第 4 作者
（88） 螺旋藻提取物对DNA拓扑异构酶活性的抑制及对DNA的直接影响, 癌症, 2000, 第 1 作者
（89） 螺旋藻提取物对DNA拓扑异构酶活性的抑制及对DNA的直接影响, 癌症：英文版, 2000, 第 5 作者
（90） 螺旋藻提取物对表皮生长因子受体酪氨酸激酶的抑制作用及诱导hl60细胞凋亡, 癌症, 2000, 第 5 作者
（91） 拓扑异构酶Ⅱ抑制剂Salvicine导致HL-60白血病细胞DNA损伤及对c-myc表达的影响, 1999, 第 1 作者
（92） 灵芝提取物对DNA拓扑异构酶的抑制作用及诱导K562细胞凋亡, 癌症, 1999, 第 4 作者

   

（ 1 ） mTOR催化抑制剂抗肿瘤作用机制的研究, 负责人, 国家任务, 2012-01--2015-12
（ 2 ） 基于PI3K亚型选择性抑制剂的肿瘤信号通路的研究, 负责人, 中国科学院计划, 2011-01--2013-12
（ 3 ） 靶向PI3K抗肿瘤药物耐药机制的研究, 负责人, 国家任务, 2014-01--2017-12
（ 4 ） 针对分子靶点的抗肿瘤药物发现及机理研究, 参与, 国家任务, 2014-01--2016-12
（ 5 ） 抗肿瘤PI3Kα选择性抑制剂CYH33的临床前研究, 负责人, 地方任务, 2014-07--2017-09
（ 6 ） “个性化药物--基于疾病分子分型的普惠新药研究”个性化药物PI3Kα选择性抑制剂CYH33临床前研究, 负责人, 中国科学院计划, 2017-01--2019-12
（ 7 ） 靶向黄嘌呤氧化酶的抗肺腺癌研究, 负责人, 国家任务, 2018-01--2021-12
（ 8 ） 组蛋白甲基转移酶EZH2介导食管鳞癌对PI3K抑制剂耐受的机制及克服策略研究, 负责人, 国家任务, 2022-01--2025-12
（ 9 ） 新PI3K抑制剂CYH33调控肿瘤免疫抗肿瘤研究, 负责人, 国家任务, 2020-01--2023-12