当前位置: X-MOL 学术J. Biomol. NMR › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Fluorine NMR functional screening: from purified enzymes to human intact living cells.
Journal of Biomolecular NMR ( IF 2.4 ) Pub Date : 2020-04-28 , DOI: 10.1007/s10858-020-00311-3
Claudio Dalvit 1 , Marina Veronesi 2 , Anna Vulpetti 3
Affiliation  

The substrate- or cofactor-based fluorine NMR screening, also known as n-FABS (n fluorine atoms for biochemical screening), represents a powerful method for performing a direct functional assay in the search of inhibitors or enhancers of an enzymatic reaction. Although it suffers from the intrinsic low sensitivity compared to other biophysical techniques usually applied in functional assays, it has some distinctive features that makes it appealing for tackling complex chemical and biological systems. Its strengths are represented by the easy set-up, robustness, flexibility, lack of signal interference and rich information content resulting in the identification of bona fide inhibitors and reliable determination of their inhibitory strength. The versatility of the n-FABS allows its application to either purified enzymes, cell lysates or intact living cells. The principles, along with theoretical, technical and practical aspects, of the methodology are discussed. Furthermore, several applications of the technique to pharmaceutical projects are presented.

中文翻译:

氟NMR功能筛选:从纯化的酶到完整的人类活细胞。

基于底物或辅因子的氟NMR筛选,也称为n-FABS(用于生化筛选的n氟原子),是执行直接功能测定以寻找酶促反应抑制剂或增强剂的有效方法。尽管与功能分析中通常使用的其他生物物理技术相比,它固有的灵敏度低,但它具有一些独特的功能,使其对于处理复杂的化学和生物系统具有吸引力。它的优势在于易于设置,坚固,灵活,缺乏信号干扰和丰富的信息含量,这些特性使您可以识别出真正的抑制剂并可靠地确定其抑制强度。n-FABS的多功能性使其可应用于纯化的酶,细胞裂解物或完整的活细胞。讨论了该方法的原理以及理论,技术和实践方面。此外,介绍了该技术在制药项目中的几种应用。
更新日期:2020-04-28
down
wechat
bug