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

J Med Chem 2002 Aug;45(18):3816-9

Ibis Therapeutics, A Division of Isis Pharmaceuticals, Inc., 2292 Faraday Avenue, Carlsbad, California 92008, USA.

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.

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http://dx.doi.org/10.1021/jm0255466DOI Listing
August 2002
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