首页> 外国专利> 2 METHOD FOR SCREENING COMPOUND BINDING TO THE ACTIVE SITE OF TARGET PROTEIN BY USING PROTEIN LABELED ON SPECIFIC AMINO ACIDS AND 2D NMR TECHNIQUE

2 METHOD FOR SCREENING COMPOUND BINDING TO THE ACTIVE SITE OF TARGET PROTEIN BY USING PROTEIN LABELED ON SPECIFIC AMINO ACIDS AND 2D NMR TECHNIQUE

机译:2通过在特定氨基酸上标记的蛋白和二维NMR技术筛选目标蛋白活性位点的化合物结合方法

摘要

PURPOSE: A method for screening a compound capable of binding to an active site of a protein using an amino acid-labeled protein and a 2D NMR technique is provided, thereby providing lead compounds for developing new medicines. CONSTITUTION: The method for screening a compound capable of binding to an active site of a protein using an amino acid-labeled protein and a 2D NMR technique comprises the steps of: (1) preparing a certain amino acid-15N or 13C labeled target protein and measuring its 2D NMR spectrum; (2) collecting known compounds, or peptides or peptide analogues capable of binding with the target protein; (3) determining the active site of a protein through binding test between the target protein-active site binding compound, target protein-peptide or target protein-peptide analogues; and (4) screening compounds showing change in the active site signal through the protein-compound binding test, wherein the target protein is an enzyme or a receptor.
机译:目的:提供一种使用氨基酸标记的蛋白质和2D NMR技术筛选能够结合至蛋白质活性位点的化合物的方法,从而提供用于开发新药物的先导化合物。组成:使用氨基酸标记的蛋白质和2D NMR技术筛选能够与蛋白质的活性位点结合的化合物的方法包括以下步骤:(1)制备某些氨基酸-15N或13C标记的目标蛋白质并测量其2D NMR光谱; (2)收集能够与靶蛋白结合的已知化合物或肽或肽类似物; (3)通过靶蛋白-活性位点结合化合物,靶蛋白-肽或靶蛋白-肽类似物之间的结合试验确定蛋白的活性位点; (4)通过蛋白质-化合物结合试验筛选显示出活性位点信号变化的化合物,其中目标蛋白质是酶或受体。

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