定点诱变——分子生物学与合理药物设计。

G Ju, E Labriola-Tompkins, T Varnell, V Madison, B Graves
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引用次数: 1

摘要

利用定点诱变技术,我们确定了I型IL-1受体(IL-1R)在人IL-1 α和IL-1 β中的结合位点的位置和组成。每个配体的结合位点是一个不连续的表位,由至少七个氨基酸组成,其侧链暴露在蛋白质表面的连续区域上。虽然人IL-1 α和IL-1 β具有相似的亲和力,并相互竞争与人I型IL-1R结合,但两种配体的结合位点残基并不相同。此外,每个配体结合位点的残基对人和小鼠IL-1R的结合有不同的贡献。IL-1结合位点的结构对IL-1拮抗剂的合理设计具有重要意义。
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Site-directed mutagenesis--molecular biology and rational drug design.

Using site-directed mutagenesis, we have determined the location and composition of the binding sites in human IL-1 alpha and IL-1 beta for the Type I IL-1 receptor (IL-1R). The binding site in each ligand is a discontinuous epitope made up of at least seven amino acids whose side chains are exposed on a contiguous region of the protein surface. Although human IL-1 alpha and IL-1 beta have similar affinities and cross-compete for binding to the human Type I IL-1R, the binding site residues are not identical in the two ligands. In addition, the residues in the binding site of each ligand contribute differently to binding of the human versus the mouse IL-1R. The structure of the IL-1 binding site has implications for the rational design of IL-1 antagonists.

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