SAR by MS: A ligand based technique for drug lead discovery against structured RNA targets

被引：111

作者：

Swayze, EE ^{[1
]}

Jefferson, EA ^{[1
]}

Sannes-Lowery, KA ^{[1
]}

Blyn, LB ^{[1
]}

Risen, LM ^{[1
]}

Arakawa, S ^{[1
]}

Osgood, SA ^{[1
]}

Hofstadler, SA ^{[1
]}

Griffey, RH ^{[1
]}

机构：

[1] Ibis Therapeut, Carlsbad, CA 92008 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 18期

关键词：

D O I：

10.1021/jm0255466

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A technique for lead discovery vs RNA targets utilizing mass spectrometry (MS) screening methods is described. The structure-activity relationships (SAR) derived from assaying weak binding motifs allows the pharmacophores discovered to be elaborated via "SAR by MS" to higher affinity ligands. Application of this strategy to a subdomain of the 23S rRNA afforded a new class of compounds with functional activity. (C) 2002 American Chemical Society.

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收藏

页码：3816 / 3819

页数：4

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