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研究生: 田鎧豪
Kai-Hau Tian
論文名稱: 氧化的穀胱甘肽類似物之全合成及生物活性評估
Total synthesis and biological evaluation of glutathione disulfide analogue
指導教授: 李文山
學位類別: 碩士
Master
系所名稱: 化學系
Department of Chemistry
論文出版年: 2005
畢業學年度: 94
語文別: 中文
中文關鍵詞: 穀胱甘肽穀氧還蛋白
論文種類: 學術論文
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  • Glutaredoxin為專門且有效地對protein-SSG進行去麩胺基硫反應(deglutathionylation)的催化蛋白質,此外,glutaredoxin也催化進行diglutathionylated HIV-1 protease的去麩胺基硫反應,使原本無活性的HIV-1 protease轉換成超活性狀態(superactive form);諸多例子指出glutaredoxin幫助恢復了麩胺基硫化蛋白質(S-glutathionylated proteins,protein-SSG)的功能,暗示glutaredoxin為體內重要的調節因子。

    有鑑於glutaredoxin提升HIV-1 protease的活性,我們便想著手設計並合成glutaredoxin的抑制劑,期望能藉由抑制glutaredoxin而阻止diglutathionylated HIV-1 protease的活化,進而發展成為理想的抗愛滋病藥物。

    另一方面,由於human glutaredoxin assay至今尚無直接的分析方法,而是採用間接的方式測得對human glutaredoxin的活性,所以我們也想在設計的分子接上發光基團,藉由偵測螢光強度建立新型、直接的human glutaredoxin assay。

    一、導論…………………………………………………………………4 1.人類穀氧還蛋白簡介…………………………………………4 2.榖胱甘肽簡介……………………………………………7 3.設計合成人類穀氧還蛋白的抑制劑…………………………8 二、結果與討論…………………………………………………………9 1.設計合成化合物30、32…………………………………………9 2.生物活性測試…………………………………………………27 三、結論…………………………………………………………………28 四、實驗與光譜數據……………………………………………………29 1.實驗儀器………………………………………………………29 2.實驗藥品………………………………………………………31 3.實驗步驟及光譜數據…………………………………………36 五、參考文獻……………………………………………………………57 六、附圖…………………………………………………………………64

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