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Development of a highly selective H2S fluorescent probe and its application to evaluate CSE inhibitors

机译:高选择性H2S荧光探针的开发及其在评估CSE抑制剂中的应用

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摘要

In this paper, we developed a novel fluorescent probe C359 for highly selective detection of H2S over other relevant biothiols. C359 is designed to contain a thiol-specific cleavable disulfide bond. H2S-mediated the disulfide cleavage and subsequent intramolecular cyclization released the masked 7-hydroxyl coumarin, displaying a remarkable fluorescence enhancement. With the promising features in hand, C359 has been applied to detect the activity of CSE (one of H2S-producing enzyme) and build up an assay for screening CSE inhibitors. We anticipated that the enzyme assay using C359 could provide a powerful methodology for screening more potent and selective enzyme inhibitors.
机译:在本文中,我们开发了一种新型荧光探针C359,可比其他相关生物硫醇进行H2S的高选择性检测。 C359设计为包含一个巯基特异性可裂解的二硫键。 H2S介导的二硫键裂解和随后的分子内环化作用释放了被掩盖的7-羟基香豆素,显示出显着的荧光增强作用。凭借具有前途的功能,C359已被应用于检测CSE(产生H2S的酶之一)的活性,并建立了用于筛选CSE抑制剂的检测方法。我们预期,使用C359的酶测定法可以为筛选更有效和选择性的酶抑制剂提供强大的方法。

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