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. Application of this strategy to a subdomain of the 23S rRNA afforded a new class of compounds with functional activity.