Literature DB >> 12190303

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

Eric E Swayze1, Elizabeth A Jefferson, Kristin A Sannes-Lowery, Lawrence B Blyn, Lisa M Risen, Satoshi Arakawa, Stephen A Osgood, Steven A Hofstadler, Richard H Griffey.   

Abstract

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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Year:  2002        PMID： 12190303     DOI： 10.1021/jm0255466

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  17 in total

1.  High throughput screening of library compounds against an oligonucleotide substructure of an RNA target.

Authors:  Karen B Gooding; Richard Higgs; Barry Hodge; Eric Stauffer; Beverly Heinz; Kevin McKnight; Krista Phipps; Michael Shapiro; Malcolm Winkler; Wai-Leung Ng; Randall K Julian
Journal:  J Am Soc Mass Spectrom       Date:  2004-06       Impact factor: 3.109

2.  A small-molecule probe induces a conformation in HIV TAR RNA capable of binding drug-like fragments.

Authors:  Amy Davidson; Darren W Begley; Carmen Lau; Gabriele Varani
Journal:  J Mol Biol       Date:  2011-07-29       Impact factor: 5.469

3.  Fragment screening of infectious disease targets in a structural genomics environment.

Authors:  Darren W Begley; Douglas R Davies; Robert C Hartley; Thomas E Edwards; Bart L Staker; Wesley C Van Voorhis; Peter J Myler; Lance J Stewart
Journal:  Methods Enzymol       Date:  2011       Impact factor: 1.600

4.  Controlling the specificity of modularly assembled small molecules for RNA via ligand module spacing: targeting the RNAs that cause myotonic muscular dystrophy.

Authors:  Melissa M Lee; Jessica L Childs-Disney; Alexei Pushechnikov; Jonathan M French; Krzysztof Sobczak; Charles A Thornton; Matthew D Disney
Journal:  J Am Chem Soc       Date:  2009-12-02       Impact factor: 15.419

5.  Discovering ligands for a microRNA precursor with peptoid microarrays.

Authors:  Sara Chirayil; Rachel Chirayil; Kevin J Luebke
Journal:  Nucleic Acids Res       Date:  2009-06-26       Impact factor: 16.971

6.  Small molecule microarrays of RNA-focused peptoids help identify inhibitors of a pathogenic group I intron.

Authors:  Lucas P Labuda; Alexei Pushechnikov; Matthew D Disney
Journal:  ACS Chem Biol       Date:  2009-04-17       Impact factor: 5.100

7.  Selection of peptides that target the aminoacyl-tRNA site of bacterial 16S ribosomal RNA.

Authors:  Mei Li; Anne-Cécile E Duc; Edvin Klosi; Srividya Pattabiraman; Mark R Spaller; Christine S Chow
Journal:  Biochemistry       Date:  2009-09-08       Impact factor: 3.162

8.  Structure of the cytosine-cytosine mismatch in the thymidylate synthase mRNA binding site and analysis of its interaction with the aminoglycoside paromomycin.

Authors:  Tony J Tavares; Alexander V Beribisky; Philip E Johnson
Journal:  RNA       Date:  2009-03-27       Impact factor: 4.942

9.  Structure of the myotonic dystrophy type 2 RNA and designed small molecules that reduce toxicity.

Authors:  Jessica L Childs-Disney; Ilyas Yildirim; HaJeung Park; Jeremy R Lohman; Lirui Guan; Tuan Tran; Partha Sarkar; George C Schatz; Matthew D Disney
Journal:  ACS Chem Biol       Date:  2013-12-16       Impact factor: 5.100

10.  Two-dimensional combinatorial screening and the RNA Privileged Space Predictor program efficiently identify aminoglycoside-RNA hairpin loop interactions.

Authors:  Dustin J Paul; Steven J Seedhouse; Matthew D Disney
Journal:  Nucleic Acids Res       Date:  2009-09-02       Impact factor: 16.971
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