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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 4898-4904 |
| Number of pages | 7 |
| Journal | Organic and Biomolecular Chemistry |
| Volume | 8 |
| Issue number | 21 |
| DOIs | |
| State | Published - Nov 7 2010 |
ASJC Scopus subject areas
- Physical and Theoretical Chemistry
- Organic Chemistry
- Biochemistry
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Schirle, N. T., Goodman, R. A., Krishnamurthy, M., & Beal, P. A. (2010). Selective inhibition of ADAR2-catalyzed editing of the serotonin 2c receptor pre-mRNA by a helix-threading peptide. Organic and Biomolecular Chemistry, 8(21), 4898-4904. https://doi.org/10.1039/c0ob00309c