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  • 學位論文

針對蛋白質激酶活性中心發展親和性化學標示之研究

Development of active site-directed affinity/alkylating probes for protein kinases

指導教授 : 羅禮強
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摘要


本論文以腺苷(adenosine)為基本架構,結合不同的親電子基團、不同長度的連接橋段建構蛋白質激酶的化學標示分子庫,利用有機合成方法,確實地合成出所設計的分子庫,並配合分子模擬計算進行蛋白質激酶:Lymphocyte protein tyrosine kinase、Focal adhesion kinase、mitogen-activated protein kinase與化學標示分子庫的對接加以驗證分子模擬計算和生化實驗的結果,篩選出具有高專一性的化學標示分子。

並列摘要


Using adenosine moiety as basic structure, we aimed at constructing a library of molecular probes for various protein kinases, including Lymphocyte protein tyrosine kinase,focal adhesion kinase, and mitogen-activated protein kinase. The construction of these probes involved the coupling of adenosine with various electrophilic groups that are linked by variable lengths of linkers. By combining the virtue of computational docking and organic syntheses, we have successfully established a library of molecular probes for the computational studies and bio-assay screening aiming at finding the highly specific probes.

並列關鍵字

protein kinase probe docking

參考文獻


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