Tether influence on the binding properties of tRNA3Lys ligands designed by a fragment-based approach

被引：54

作者：

Moumne, Roba ^{[1
]}

Larue, Valery ^{[2
]}

Seijo, Bili ^{[2
]}

Lecourt, Thomas ^{[1
]}

Micouin, Laurent ^{[1
]}

Tisne, Carine ^{[2
]}

机构：

[1] Univ Paris 05, CNRS UMR 8638, F-75006 Paris, France

[2] Univ Paris 05, Cristallog & RMN Biol, CNRS UMR 8015, F-75006 Paris, France

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2010年 / 8卷 / 05期

关键词：

HIV-1 REVERSE TRANSCRIPTION; CLICK CHEMISTRY; 1,3-DIPOLAR CYCLOADDITION; MEDICINAL CHEMISTRY; ESCHERICHIA-COLI; NMR-SPECTROSCOPY; TERMINAL ALKYNES; SMALL MOLECULES; LEAD DISCOVERY; POWERFUL TOOL;

D O I：

10.1039/b921232a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A small library of 1,5-triazole derivatives linking a diaminocyclopentadiol and aromatic ketones has been prepared and screened using NMR and fluorescent techniques against tRNA(3)(Lys), the HIV reverse transcription primer. The comparison of their binding properties to those of their 1,4-triazole isomers, previously discovered in a fragment-based approach, outlines the influence of the linker on affinity and binding selectivity in such an approach.

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收藏

页码：1154 / 1159

页数：6

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