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

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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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0255466