Spy vs. spy: selecting the best reporter for 19F NMR competition experiments

被引:22
|
作者
de Castro, Guilherme Vieira [1 ]
Ciulli, Alessio [1 ]
机构
[1] Univ Dundee, Sch Life Sci, Div Biol Chem & Drug Discovery, Dow St, Dundee DD1 5EH, Scotland
基金
欧洲研究理事会; 英国惠康基金;
关键词
E3 UBIQUITIN LIGASE; PROTEIN-PROTEIN INTERACTION; STRUCTURE-GUIDED DESIGN; SMALL MOLECULES; DRUG DISCOVERY; LEAD DISCOVERY; AFFINITY; OPTIMIZATION; LIBRARY; BINDING;
D O I
10.1039/c8cc09790a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Systematic characterization of a series of fluorinated VHL ligands, varying binding affinity and position of the trifluoromethyl group, qualifies a spy molecule for competitive F-19 NMR screening and reveals guiding principles to develop highly sensitive assays with low material consumption.
引用
收藏
页码:1482 / 1485
页数:4
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