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標題: | 合成含仿磷酸酪胺酸基團之Diketopiperazine分子庫 Synthesis of Phosphotyrosine Mimetic-Containing Diketopiperazines |
作者: | Yun-Ting Chou 周昀亭 |
指導教授: | 羅禮強(Lee-Chiang Lo) |
關鍵字: | 仿磷酸酪胺酸基團, diketopiperazine,phosphotyrosine mimics, |
出版年 : | 2011 |
學位: | 碩士 |
摘要: | Diketopiperazines由於含有獨特的雜環體系,因而存在著各式各樣的生物活性,本論文中,目標是建構一個帶有仿磷酸酪胺酸基團之diketopiperazine組合式分子庫,而兩組線性型式雙胜肽(Fmoc-X-cpY-OMe and Fmoc-cpY-X-NH2)也同時合成出做為對照研究的目的,這裡X代表19個胺基酸殘基和11個側鏈有保護的氨基酸,而cpY代表仿磷酸酪胺酸殘基,因此,分子庫是由三個子集組合而成,包含31個diketopierazines、31個Fmoc-X-cpY-OMe以及28個Fmoc-cpY-X-NH2,共90個化合物個別製備完成,此分子庫對於各酵素家族做為抑制劑之篩選目前已在進行中,包括蛋白質酪胺酸磷酯質水解酶和激酶。 Diketopiperazines have a wide variety of biological activities due to their peculiar heterocyclic system. In this thesis, we aimed to construct a combinatorial library of diketopiperazines carrying a phosphotyrosine mimetic group. For the purpose of comparative study, two linear forms of dipeptides (Fmoc-X-cpY-OMe and Fmoc-cpY-X-NH2) were also synthesized. Here X stands for the 19 amino acid residues and for the 11 side chain-protected amino acids; whereas cpY stands for the phosphotyrosine mimetic residue. Therefore, the library is composed of three subsets. Totally, 90 compounds were individually prepared, including 31 diketopierazines, 31 Fmoc-X-cpY-OMe, and 28 Fmoc-cpY-X-NH2. This molecular library is currently being screened for inhibitors toward various enzyme families, including protein tyrosine phosphatases and kinases. |
URI: | http://tdr.lib.ntu.edu.tw/jspui/handle/123456789/23164 |
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顯示於系所單位: | 化學系 |
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ntu-100-1.pdf 目前未授權公開取用 | 42.37 MB | Adobe PDF |
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