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

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2007年 / 46卷 / 24期

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

页码：4489 / 4491

页数：3

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