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氘和氚标记化合物:在生命科学中的应用。

Deuterium- and Tritium-Labelled Compounds: Applications in the Life Sciences.

机构信息

Isotope Chemistry and Metabolite Synthesis, Integrated Drug Discovery, Medicinal Chemistry, Industriepark Höchst, G876, 65926, Frankfurt, Germany.

Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral Street, Glasgow, Scotland, G1 1XL, UK.

出版信息

Angew Chem Int Ed Engl. 2018 Feb 12;57(7):1758-1784. doi: 10.1002/anie.201704146. Epub 2018 Jan 4.

DOI:10.1002/anie.201704146
PMID:28815899
Abstract

Hydrogen isotopes are unique tools for identifying and understanding biological and chemical processes. Hydrogen isotope labelling allows for the traceless and direct incorporation of an additional mass or radioactive tag into an organic molecule with almost no changes in its chemical structure, physical properties, or biological activity. Using deuterium-labelled isotopologues to study the unique mass-spectrometric patterns generated from mixtures of biologically relevant molecules drastically simplifies analysis. Such methods are now providing unprecedented levels of insight in a wide and continuously growing range of applications in the life sciences and beyond. Tritium ( H), in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery. The efforts and costs associated with the synthesis of labelled compounds are more than compensated for by the enhanced molecular sensitivity during analysis and the high reliability of the data obtained. In this Review, advances in the application of hydrogen isotopes in the life sciences are described.

摘要

氢同位素是识别和理解生物和化学过程的独特工具。氢同位素标记允许在有机分子中无痕且直接掺入额外的质量或放射性标记,而几乎不会改变其化学结构、物理性质或生物活性。使用氘标记的同位素来研究从生物相关分子混合物中产生的独特质谱模式,可以极大地简化分析。这些方法现在在生命科学及其他领域的广泛且不断增长的应用中提供了前所未有的洞察力。特别是氚 ( H) 的使用有所增加,特别是在药物发现中。在分析过程中增强的分子灵敏度以及获得的数据的高可靠性,超过了标记化合物合成相关的努力和成本。在这篇综述中,描述了氢同位素在生命科学中的应用进展。

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