SAR by MS: A Ligand Based Technique for Drug Lead Discovery Against Structured RNA Targets

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. Applic...

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Veröffentlicht in:	Journal of medicinal chemistry 2002-08, Vol.45 (18), p.3816-3819
Hauptverfasser:	Swayze, Eric E, Jefferson, Elizabeth A, Sannes-Lowery, Kristin A, Blyn, Lawrence B, Risen, Lisa M, Arakawa, Satoshi, Osgood, Stephen A, Hofstadler, Steven A, Griffey, Richard H
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acids - chemistry Biological and medical sciences Ligands Mass Spectrometry Medical sciences Miscellaneous Pharmacology. Drug treatments Quantitative Structure-Activity Relationship Quinoxalines - chemistry RNA - chemistry Stereoisomerism
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container_end_page	3819
container_issue	18
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container_title	Journal of medicinal chemistry
container_volume	45
creator	Swayze, Eric E Jefferson, Elizabeth A Sannes-Lowery, Kristin A Blyn, Lawrence B Risen, Lisa M Arakawa, Satoshi Osgood, Stephen A Hofstadler, Steven A Griffey, Richard H
description	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.
doi_str_mv	10.1021/jm0255466
format	Article
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subjects	Amino Acids - chemistry Biological and medical sciences Ligands Mass Spectrometry Medical sciences Miscellaneous Pharmacology. Drug treatments Quantitative Structure-Activity Relationship Quinoxalines - chemistry RNA - chemistry Stereoisomerism
title	SAR by MS: A Ligand Based Technique for Drug Lead Discovery Against Structured RNA Targets
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