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Non-invasive 19F NMR analysis of a protein-templated N-acylhydrazone dynamic combinatorial library
Organic & Biomolecular Chemistry ( IF 3.2 ) Pub Date : 2018-10-04 , DOI: 10.1039/c8ob01918e
Alexander G. Ekström 1, 2, 3, 4 , Jue Theresa Wang 1, 2, 3, 4 , Juraj Bella 1, 2, 3, 4 , Dominic J. Campopiano 1, 2, 3, 4
Affiliation  

Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets. We used 19F NMR as an in situ, non-invasive technique for measuring the composition of a dynamic combinatorial library (DCL) of N-acylhydrazones (NAHs). An NAH DCL, constructed from a fluoro-aromatic aldehyde and a small set of hydrazides, was targetted at ecFabH, an essential enzyme in bacterial fatty acid biosynthesis. Our NMR analysis identified a tert-butyl NAH as the best binder which was confirmed by enzymatic assay.

中文翻译:

蛋白质模板化N-酰基hydr动态组合文库的非侵入式19 F NMR分析

动态组合化学(DCC)是识别生物靶标配体的强大工具。我们使用19 F NMR作为原位非侵入性技术来测量N-酰基hydr(NAHs)的动态组合文库(DCL)的组成。由氟代芳族醛和少量酰肼构成的NAH DCL靶向ec FabH,它是细菌脂肪酸生物合成中必不可少的酶。我们的NMR分析确定了丁基NAH是最好的粘合剂,这已通过酶法测定得到了证实。
更新日期:2018-11-07
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