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氟修饰核酸的合成及其生物学应用

Synthesis and biological applications of fluoro-modified nucleic acids.

作者信息

Guo Fengmin, Li Qiang, Zhou Chuanzheng

机构信息

State Key Laboratory of Elemento-Organic Chemistry and Department of Chemical Biology, College of Chemistry, Nankai University, Tianjin 300071, China.

出版信息

Org Biomol Chem. 2017 Nov 22;15(45):9552-9565. doi: 10.1039/c7ob02094e.

Abstract

Owing to the unique physical properties of a fluorine atom, incorporating fluoro-modifications into nucleic acids offers striking biophysical and biochemical features, and thus significantly extends the breadth and depth of biological applications of nucleic acids. In this review, fluoro-modified nucleic acids that have been synthesized through either solid phase synthesis or the enzymatic approach are briefly summarised, followed by a section describing their biomedical applications in nucleic acid-based therapeutics, F PET imaging and mechanistic studies of DNA modifying enzymes. In the last part, the utility of F NMR and MRI for probing the structure, dynamics and molecular interactions of fluorinated nucleic acids is reviewed.

摘要

由于氟原子独特的物理性质,将氟修饰引入核酸可提供显著的生物物理和生化特性,从而极大地扩展了核酸生物应用的广度和深度。在本综述中,简要总结了通过固相合成或酶促方法合成的氟修饰核酸,随后介绍了它们在基于核酸的治疗、氟正电子发射断层显像(F PET)成像以及DNA修饰酶的机制研究中的生物医学应用。在最后一部分,综述了氟核磁共振(F NMR)和磁共振成像(MRI)在探测氟化核酸的结构、动力学和分子相互作用方面的应用。

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