沈建华 - 中国科学院上海药物研究所 -

个人简介

教育经历 1995-1998 复旦大学获物理学理学博士学位 1992-1995 西安交通大学获电子工程专业工学硕士学位 1983-1987 国防科技大学获材料科学专业工学学士学位工作经历 2004-至今中科院上海药物研究所课题组长、研究员、博导 2002-2004 中科院上海药物研究所课题组长、研究员 2000-2002 中科院上海药物研究所副研究员 1998-2000 中科院上海药物研究所博士后 1987-1992 航天局165厂技术员、工程师

研究领域

1. 多囊肾病治疗药物发现与临床前研究 2. 糖尿病新药发现与优化 3. 动脉粥样硬化药物发现 4. 神经精神类疾病药物发现

近期论文

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Triazole derivatives: a series of Darapladib analogues as orally active Lp-PLA2 inhibitors.Wang K, Xu W, Zhang W, Mo M, Wang Y, Shen J. Bioorg Med Chem Lett. 2013 May 15;23(10):2897-901. Design and synthesis of imidazole and triazole derivatives as Lp-PLA₂ inhibitors and the unexpected discovery of highly potent quaternary ammonium salts.Wang K, Xu W, Liu Y, Zhang W, Wang W, Shen J, Wang Y. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1187-92. Inhibition of lipoprotein-associated phospholipase A2 ameliorates inflammation and decreases atherosclerotic plaque formation in ApoE-deficient mice.Wang WY, Zhang J, Wu WY, Li J, Ma YL, Chen WH, Yan H, Wang K, Xu WW, Shen JH, Wang YP. PLoS One. 2011;6(8):e23425. Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors. Yang H, Shen Y, Chen J, Jiang Q, Leng Y, Shen J. Eur J Med Chem. 2009 Mar;44(3):1167-71. Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro. Zhang X, Zhou Y, Shen Y, Du LL, Chen JH, Leng Y, Shen JH. Acta Pharmacol Sin. 2009 Sep;30(9):1344-50. Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.Ye YL, Zhou Z, Zou HJ, Shen Y, Xu TF, Tang J, Yin HZ, Chen ML, Leng Y, Shen JH.Bioorg Med Chem. 2009 Aug 1;17(15):5722-32. 4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice. Zhang X, Zhou Z, Yang H, Chen J, Feng Y, Du L, Leng Y, Shen J. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4455-8. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Feng Y, Huang SL, Dou W, Zhang S, Chen JH, Shen Y, Shen JH, Leng Y.Br J Pharmacol. 2010 Sep;161(1):113-26. Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice. Zhang L, Chen J, Ning M, Zou Q, Leng Y, Shen J. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2748-52. 4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists. Zou Q, Duan H, Ning M, Liu J, Feng Y, Zhang L, Zhu J, Leng Y, Shen J. Eur J Med Chem. 2014 May 13;82C:1-15. Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold. Zhu J, Ning M, Guo C, Zhang L, Pan G, Leng Y, Shen J. Eur J Med Chem. 2013 Nov;69:55-68. Design, synthesis, and structure-activity relationships of 3,4,5-trisubstituted 4,5-dihydro-1,2,4-oxadiazoles as TGR5 agonists. Zhu J, Ye Y, Ning M, Mándi A, Feng Y, Zou Q, Kurtán T, Leng Y, Shen J. ChemMedChem. 2013 Jul;8(7):1210-23. Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. Duan H, Ning M, Chen X, Zou Q, Zhang L, Feng Y, Zhang L, Leng Y, Shen J. J Med Chem. 2012 Dec 13;55(23):10475-89.