| 人胰酶抑制剂的固相合成 |
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| 引用本文： | 王恩思,船越奖.人胰酶抑制剂的固相合成[J].高等学校化学学报,1990,11(8):837-842. |
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| 作者姓名： | 王恩思 船越奖 |
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| 作者单位： | 吉林大学分子生物学系
(王恩思，徐坚平，王宗睦，李惟)，日本京都大学药学部
(船越奖)，日本京都大学药学部(矢岛治明) |
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| 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TMSOT_t-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％。
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| 关 键 词： | 人胰酶抑制剂 固相合成 |
Solid Phase Synthesis of the Human Trypsin Inhibitor |
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| Wang Ensi,Xu Jianping,Wang Zongmu,Li Wei.Solid Phase Synthesis of the Human Trypsin Inhibitor[J].Chemical Research In Chinese Universities,1990,11(8):837-842. |
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| Authors: | Wang Ensi Xu Jianping Wang Zongmu Li Wei |
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| 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. TMSOT1-thioanisol/TFA have been used as the agent which cleaves HTI from the resin and removes all of the side chain protecting groups simultaneously. Crude HTI was 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. |
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| Keywords: | Human trypsin inhibitor Solid phase peptide synthesis Trimethylsilyl trifluoromethane-sulf onate (TMSOT1) |
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