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Modified tumor necrosis factor-alpha converting enzyme and methods of use thereof

机译:修饰的肿瘤坏死因子-α转化酶及其使用方法

摘要

The present invention discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.
机译:本发明公开了一种修饰的肿瘤坏死因子-α转化酶(TACE)催化结构域,其不同于天然的TACE催化结构域,在高蛋白质浓度下是稳定的。本发明进一步公开了在具有多种抑制剂的蛋白质-配体复合物中产生修饰的TACE蛋白质的晶体的方法。另外,本发明公开了使用获得的蛋白质,晶体和/或三维结构来鉴定可调节TACE酶活性的化合物的方法。

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