基本信息
刘东祥  男  博导  中国科学院上海药物研究所
电子邮件: dxl@mail.shcnc.ac.cn
通信地址: 上海市浦东祖冲之路555号
邮政编码: 201203

招生信息

   
招生专业
1007Z1-药物设计学
100706-药理学
招生方向
蛋白质化学
药物设计
癌症, 神经退行性疾病, 糖尿病

教育背景

1995-09--1998-07   中国科学院上海药物所   博士
1992-09--1995-08   上海市同济大学   硕士
1987-09--1992-08   上海市同济大学   学士

工作经历

   
工作简历
2005-06~2011-07,中国科学院上海药物研究所, 教授
2004-06~2005-05,The Burnham Institute, California, U.S.A., Research Assistant Professor
2002-01~2004-05,University of Illinois at Urbana-Champaign, Research Scientist
1998-08~2001-12,Thomas Jefferson University, Philadelphia, U.S.A, Postdoctor
1995-09~1998-07,中国科学院上海药物所, 博士
1992-09~1995-08,上海市同济大学, 硕士
1987-09~1992-08,上海市同济大学, 学士

专利与奖励

   
专利成果
( 1 ) 阻止阿尔茨海默氏症Abeta多肽纤维化的小分子抑制剂及其制备方法、药物组合和应用, 2011, 第 1 作者, 专利号: ZL 2006 1 0028555.2
( 2 ) 喹唑啉-2(1H)吡啶硫酮类衍生物、其药物组合物、制备方法及应用, 2010, 第 1 作者, 专利号: 201010128391.7
( 3 ) 以3-苯甲酰-1-苯并呋喃为骨架的新一类SIRT1小分子抑制剂在制备治疗或预防癌症及与蛋白去乙酰化相关的疾病的药物方面的用途, 2010, 第 1 作者, 专利号: 201010254379.0

出版信息

   
发表论文
(1) Structural basis for the interaction of diapause hormone with its receptor in the silkworm, Bombyx mori, FASEB Journal, 2018, 通讯作者
(2) Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase., Acta Pharm Sin B., 2016, 通讯作者
(3) Crystal Structures of SIRT3 Revealed that the a2-a3 Loop and a3-Helix Affect the Interaction of Long-Chain Acyl Lysine, FEBS Letters, 2016, 通讯作者
(4) Structural basis for allosteric, substrate-dependent stimulation of SIRT1 activity by resveratrol, Genes & Development, 2015, 第 4 作者
(5) Structure-activity relationship and interaction studies of new SIRT1 inhibitors with the scaffold of 3-(furan-2-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole., Bioorg Med Chem Lett., 2014, 通讯作者
(6) Integration and oligomerization of Bax protein in lipid bilayers characterized by single molecule fluorescence study, Journal of Biological Chemistry, 2014, 通讯作者
(7) Identification of benzofuran-3-yl (phenyl)methanones as novel SIRT1 inhibitors: binding mode, inhibitory mechanism and biological action, European Journal of Medicinal Chemistry, 2013, 通讯作者
(8) Discovery and Mechanism Study of SIRT1 Activators that Promote the Deacetylation of Fluorophore-Labeled Substrate, Journal of Medicinal Chemistry, 2013, 通讯作者
(9) Computational screening for active compounds targeting protein sequences: methodology and experimental validation, Journal of Chemical Information and Modeling, 2011, 第 2 作者
(10) Structural Optimization and Biological Evaluation of Substituted Bisphenol A Derivatives as beta-Amyloid Peptide Aggregation Inhibitors, Journal of Medicinal Chemistry, 2010, 通讯作者
(11) Design, Synthesis and Interaction Study of Quinazoline-2(1H)-Thione Derivatives as Novel Bcl-xL Inhibitors, Journal of Medicinal Chemistry, 2010, 通讯作者
(12) An enzyme-linked immunosorbent assay to compare the affinity of chemical compounds for beta-amyloid peptide as a monomer, Analytical and Bioanalytical Chemistry, 2010, 通讯作者
(13) Dual role of Zn2+ in maintaining structural integrity and suppressing deacetylase activity of SIRT1, Journal of Inorganic Biochemistry, 2010, 通讯作者
(14) Structure assembly of Bcl-xL through a5-a5 and b6-b6 interhelix interactions in lipid membranes, Biochimica et Biophysica Acta-Biomembranes, 2009, 通讯作者
(15) A fluorometric assay of SIRT1 deacetylation activity through quantification of nicotinamide adenine dinucleotide, Analytical Biochemistry, 2009, 通讯作者
(16) A conserved hydrophobic core at Bcl-xL mediates its structural stability and binding affinity with BH3-domain peptide of pro-apoptotic protein, Archives of Biochemistry and Biophysics, 2009, 通讯作者
(17) A new assay based on fluorescence resonance energy transfer to determine the binding affinity of Bcl-xL inhibitors, Bioscience Biotechnology and Biochemistry, 2008, 通讯作者
(18) Bcl-xL forms two distinct homodimers at non-ionic detergents: implications in the dimerization of Bcl-2 family proteins., Journal of Biochemistry, 2008, 通讯作者

科研活动

   
科研项目
( 1 ) 具有干细胞调控活性的天然产物的挑选和收集, 主持, 国家级, 2009-09--2013-12
( 2 ) 细胞凋亡调控因子Bcl-xL、Bax、tBid的相互作用、构象变化和寡聚行为研究, 主持, 国家级, 2015-01--2018-12
( 3 ) 基于sirtuins酶结构的化学探针设计, 主持, 国家级, 2017-01--2020-12