高等学校化学学报 ›› 2006, Vol. 27 ›› Issue (4): 669.

• 研究简报 • 上一篇    下一篇

新型含硫肿瘤坏死因子类肽抑制剂的合成与活性

王鼎, 张奇涵, 许家喜   

  1. 北京大学化学与分子工程学院, 生物有机与分子工程教育部重点实验室, 北京 100871
  • 收稿日期:2005-05-09 出版日期:2006-04-10 发布日期:2006-04-10
  • 通讯作者: 许家喜(1963年出生), 男, 博士, 教授, 从事有机合成化学研究. E-mail: jxxu@pku.edu.cn
  • 基金资助:

    国家自然科学基金(批准号: 20472005)资助

Synthesis and Activity of Novel Sulfur-containing Peptidomimetic Inhibitors of Tumor Necrosis Factor

WANG Ding, ZHANG Qi-Han, XU Jia-Xi*   

  1. Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education,
    College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
  • Received:2005-05-09 Online:2006-04-10 Published:2006-04-10
  • Contact: XU Jia-Xi,E-mail: jxxu@pku.edu.cn

摘要:

为了发展新型TNF类肽抑制剂, 考虑到酶活性中心含有Zn2+离子, 我们以通式1的骨架为基础, 设计并合成了一类含有硫原子的类肽化合物2, 其具有三肽的基本骨架, 羟胺的游离羟基和侧链上的硫原子均可与金属蛋白酶活性中心的Zn2+络合, 起抑制活性作用.

关键词: 肿瘤坏死因子; 多肽; 类肽抑制剂

Abstract:

Tumor necrosis factor is one of the important cell factors, which can regulate pro-imflammatory. On the basis of the known and efficient peptidomimetic inhibitors of tumor necrosis factor as the leading compounds, novel sulfur-containing peptidomimetic inhibitors were designed and synthesized in a convenient and efficient manner. Bioassay results indicate that three of them showed some inhibition activity on sTNF-α secretion in HL-60 cells induced by lipolysaccharide, and two of them showed a good stability and inhibition activity.

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