NMR-Guided fragment-based approach for the design of tRNALys3 ligands

被引:36
作者
Chung, Florence [1 ]
Tisne, Carine [1 ]
Lecourt, Thomas [1 ]
Dardel, Frederic [1 ]
Micouin, Laurent [1 ]
机构
[1] Univ Paris 05, CNRS, Cristallogr & RMN Biol, F-75006 Paris, France
关键词
aminoglycoside mimics; drug design; fragment-based synthesis; RNA recognition; tRNA;
D O I
10.1002/anie.200605201
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Two in one: Two ligands for tRNALys3 that were identified from a compound library by flow-injection NMR spectroscopic screening and found to have millimolar dissociation constants (on the left in the picture) inspired the fragment-based synthesis of a new family of ligands with the general structural features of both initial compounds. Ligand 1 of this family is a selective D-stem binder of tRNALys3 with a micromolar Kd value. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:4489 / 4491
页数:3
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