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      當前位置:科學網首頁 > 基金首頁 > GD3s的表達、調控及作用機制研究

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      GD3s的表達、調控及作用機制研究

      批準號81703565 學科分類抗腫瘤藥物藥理 ( H3105 )
      項目負責人富煒琦 負責人職稱助理研究員 依托單位中國醫學科學院藥物研究所
      資助金額20.10
      萬元
      項目類別青年科學基金項目 研究期限2018 年 01 月 01 日 至
      2020 年 12 月 31 日
      中文主題詞腫瘤侵襲和轉移;神經節苷脂;GD3合成酶;藥物靶點;高通量藥物篩選
      英文主題詞tumor invasion and metastasis;gangliosides;GD3 synthase;drug target; high-throughput drug screening

      摘要

      中文摘要 癌癥發病率與死亡率持續上升。癌癥已成為我國死亡的主要原因。神經節苷脂GD3 及其下游產物GD2在癌癥發生、發展中發揮重要作用。GD3合成酶(GD3 synthase,GD3s)是合成GD3的唯一關鍵酶,GD3s在腫瘤的侵襲和遷移中發揮重要的作用。目前GD3s的活性位點及催化機制還是不清楚,也沒有它的抑制劑。我們構建了GD3s真核表達質粒和原核表達質粒并表達具有活性的GD3s蛋白,并利用該活性蛋白建立基于酶催化的高通量篩選模型。我們認為GD3s是個潛在的重要藥物靶點,其抑制劑對治療癌癥具有重要意義。本研究將利用生物信息學,分子生物學和生物物理學的技術方法對GD3s的結構和功能展開研究,進一步確定GD3s為腫瘤潛在重要靶點;建立同源模型進行虛擬篩選結合基于酶催化的高通量篩選模型篩選GD3s抑制劑。GD3s的活性位點確立、催化機制的闡明及GD3s抑制劑的發現對癌癥的發現和治療具有重要意義。
      英文摘要 Cancer incidence and mortality rates continue to rise. Cancer has become the main cause of death in China. Ganglioside GD3 and its downstream product GD2 play important roles in the occurrence and development of cancer. GD3 synthase (GD3s) is the only key enzyme in the synthesis of GD3, which plays an important role in tumor invasion and migration. So far, the active site and catalytic mechanism of GD3s are still unclear, and there are no GD3s inhibitors. We constructed GD3s eukaryotic expression plasmid and prokaryotic expression plasmid and expressed the active GD3s protein, and established a high throughput screening model based on enzyme catalysis. We propose that GD3s is an important drug target, and its inhibitors are of great significance in the treatment of cancer. In this study we will use multiple methods of bioinformatics, molecular biology and biophysics to study the structure and function of GD3s, to further determine that GD3s is a potential tumor target. Besides, we will establish virtual screening based on computation modeling, combined with high-throughput screening model based on enzyme catalysis, to screen GD3s inhibitors. The determination of the active site of GD3s, the elucidation of the catalytic mechanism and the discovery of GD3s inhibitors are of great significance to the diagnosis and treatment of cancer.
      結題摘要

      成果

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