頁籤選單縮合
題名 | Application of BIA Technology in Screening Potential MAT Inhibitors= |
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作者 | 陳惠明; 黃麗嬌; 張昱勛; 陳慧毅; 龍鳳娣; 郭盛助; Chen, Hui-ming; Huang, Li-jiau; Chang, Yu-hsun; Chen, Huey-yi; Lung, Feng-di T.; Kuo, Sheng-chu; |
期刊 | 中華藥學雜誌 |
出版日期 | 20010600 |
卷期 | 53:3 2001.06[民90.06] |
頁次 | 頁147-155 |
分類號 | 418.1 |
語文 | eng |
關鍵詞 | Methylation; Methionine adenosyl transferase; MAT; Methionine; BIA; Biomolecular interaction analysis; Radiolabeled method; |
英文摘要 | Alterations in DNA methylation are very common in cancer cells. The exploration of methylation inhibitors based on their inhibition of methionine adenosyl transferase (MAT) is important in the search for antitumor agents. For efficient screening of potential MAT inhibitors, we developed a preliminary screening method based on biomolecular interaction analysis (BIA) technology to detect interactions between synthetic compounds and MAT. We also compared the BIA method with the conventional radiolabeled method to evaluate its efficacy for screening potential MAT inhibitors. Using the BIA method, D-methionine and indoleacetic acid could be excluded as candidate inhibitors (exclusion rate = 2/5) since they only weakly inhibited MAT binding to immobilized methionine (D-methionine: 1 mM, DRU2/DRU1 = 0.202; Indoleacetic acid: 2 mM, DRU2/DRU1 = 0.202). The inhibitory effect of the potential MAT inhibitors was also assessed using the radiolabeled method and it was reconfirmed that D-methionine and indoleacetic acid were poor inhibitors. The sensitivity, specificity, positive predictive value, and negative predictive value of screening potential MAT inhibitors using the BIA method were 100 %, 66.6 %, 66.6 %, and 100 %, respectively. The present study demonstrates that an efficient method for screening potential MAT inhibitors was established using the BIA technology. |
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