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PEGylated substrates of NSP4 protease: A tool to study protease specificity

机译:NSP4蛋白酶的聚乙二醇化底物:一种研究蛋白酶特异性的工具

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Herein we present the synthesis of a novel type of peptidomimetics composed of repeating diaminopropionic acid residues modified with structurally diverse heterobifunctional polyethylene glycol chains (abbreviated as DAPEG). Based on the developed compounds, a library of fluorogenic substrates was synthesized. Further library deconvolution towards human neutrophil serine protease 4 (NSP4) yielded highly sensitive and selective internally quenched peptidomimetic substrates. In silico analysis of the obtained peptidomimetics revealed the presence of an interaction network with distant subsites located on the enzyme surface.
机译:在本文中,我们介绍了一种新型肽模拟物,这些肽模拟物组成,这些肽二酸残基与在结构各样的异双官能聚乙二醇链(缩写为DAPEG)中修饰的二氨基丙酸残基组成。基于开发的化合物,合成了一种荧光底物库。进一步的图书馆去卷积朝向人嗜中性粒细胞丝氨酸蛋白酶4(NSP4)产生高度敏感和选择性的内部猝灭的拟肽底物。在所获得的肽模拟物的硅分析中,揭示了位于酶表面上的远处底座的相互作用网络的存在。

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