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首页> 外文期刊>RSC Advances >Fluorescent analogs of cyclic and linear dinucleotides as phosphodiesterase and oligoribonuclease activity probes
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Fluorescent analogs of cyclic and linear dinucleotides as phosphodiesterase and oligoribonuclease activity probes

机译：环状和线性二核苷酸的荧光类似物，作为磷酸二酯酶和寡核糖核酸酶活性探针

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Cyclic dinucleotide-based second messengers, including c-di-GMP, c-di-AMP and cGAMP, are universal signaling molecules widely used by prokaryotes and eukaryotes. C-di-GMP and c-di-AMP play key roles in bacterial survival. Consequently, metabolism proteins that modulate cyclic dinucleotide concentrations, such as cyclic dinucleotide phosphodiesterases (PDE), are potential drug targets; thus, probes that report PDE activity could have great utility in high throughput screening for PDE inhibitors. However, there is a paucity of luminescent-based probes for monitoring cyclic dinucleotide PDE activity. In this study, we synthesized various fluorescent nucleobase (ethenoA and 2-AP) analogs of cyclic and linear dinucleotides. These analogs were readily cleaved by the cyclic dinucleotide PDE and oligoribonucleases (Orn). Cleavage of the fluorescent probes led to changes in fluorescence intensities. Our results suggest that these fluorescent analogs can be used to monitor the activity of cyclic dinucleotide PDEs in real time and that these probes could facilitate the identification of inhibitors of cyclic dinucleotide PDEs. Additionally these probes could be used to profile the activity of expressed PDEs and Orns.
机译：基于环二核苷酸的第二信使，包括c-di-GMP，c-di-AMP和cGAMP，是原核生物和真核生物广泛使用的通用信号分子。 C-di-GMP和c-di-AMP在细菌存活中起关键作用。因此，调节环状二核苷酸浓度的代谢蛋白，例如环状二核苷酸磷酸二酯酶（PDE），是潜在的药物靶点。因此，报告PDE活性的探针可能在PDE抑制剂的高通量筛选中具有很大的用途。然而，缺乏用于监测环状二核苷酸PDE活性的基于发光的探针。在这项研究中，我们合成了环状和线性二核苷酸的各种荧光核碱基（ethenoA和2-AP）类似物。这些类似物很容易被环状二核苷酸PDE和寡核糖核酸酶（Orn）裂解。荧光探针的切割导致荧光强度的变化。我们的结果表明，这些荧光类似物可用于实时监测环二核苷酸PDEs的活性，并且这些探针可以促进环二核苷酸PDEs抑制剂的鉴定。另外，这些探针可用于分析表达的PDE和Orns的活性。

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