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Org Biomol Chem. 2010 Nov 7;8(21):4898-904. doi: 10.1039/c0ob00309c. Epub 2010 Aug 31.

Selective inhibition of ADAR2-catalyzed editing of the serotonin 2c receptor pre-mRNA by a helix-threading peptide.

Author information

1
Department of Chemistry, University of California, Davis, CA 95616, USA.

Abstract

RNA editing by adenosine deamination is a form of epigenetic control of gene expression wherein the ADAR enzymes convert adenosine to inosine in RNA often changing the meaning of codons. The pre-mRNA for the 2c subtype of serotonin receptor (5-HT2cR) is shown here to support small molecule binding near known editing sites. Furthermore, a helix-threading peptide binds this site and inhibits the in vitro reaction of ADAR2 in an RNA-substrate selective manner. This is the first example of substrate-selective inhibition of editing by an RNA-binding small molecule and sets the stage for the development of new reagents capable of controlling gene function through manipulation of mRNA editing.

PMID:
20820662
DOI:
10.1039/c0ob00309c
[Indexed for MEDLINE]

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