高等学校化学学报

高等学校化学学报 ›› 1990, Vol. 11 ›› Issue (8): 837.

• 研究论文 • 上一篇    下一篇

人胰酶抑制剂的固相合成

王恩思1, 徐坚平1, 王宗睦1, 李惟1, 船越奖2, 矢岛治明2   

  1. 1. 吉林大学分子生物学系;
    2. 日本京都大学药学部
  • 收稿日期:1989-06-01 出版日期:1990-08-24 发布日期:1990-08-24
  • 通讯作者: 王宗睦
  • 基金资助:

    国家自然科学基金

Solid Phase Synthesis of the Human Trypsin Inhibitor

Wang Ensi1, Xu Jianping1, Wang Zongmu1, Li Wei1, S. Funakoshi2, H. Yajima2   

  1. 1. Department of Molecular Biology, Jilin University, Changchun;
    2. Faculty of Phamaceutical Science, Kyoto University, Kyoto, Japan
  • Received:1989-06-01 Online:1990-08-24 Published:1990-08-24

PDF (PC)

被引次数

5

摘要： 本文用固相多肽合成法以逐步和片段缩合并用的方武首次合成了人胰酶抑制剂,其中采用了TMSOTf-硫代茴香醚/TFA糸统切断载体-肽的连接键及脱除全部侧链保护基,合成产物经脱氢胰酶亲合层析与HPLC精制,总产率6.3%.合成品对牛胰酶有很强的抑制能力,其活性约为天然产物的97%。

关键词: 人胰酶抑制剂, 固相多肽合成, 三氟甲磺酸三甲基硅烷酯

Abstract: This paper describes synthesis of the human trypsin inhibitor (HTI) by the solid phase method in which both stepwise and segment condensation are involved. TMSOTf-thioanisol/TFA have been used as the agent which cleaves HTIfrom the resin and removes all of the side chain protecting groups simultaneously. Crude HTIwas purified by affinity chromatography on anhydro- trypsinr sepharose and reverse phase HPLC, the total yield is 6.3%. The resulting product shows powerful trypsin inhibitory activity that near 97% of the activity of natural HTI.

Key words: Human trypsin inhibitor, Solid phase peptide synthesis, Trimethylsilyl trifluoromethane-sulf onate (TMSOTf)

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