期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 8, 期 21, 页码 4898-4904出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0ob00309c
关键词
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资金
- National Institutes of Health [R01-GM061115]
- NIGMS-NIH [T32-GM08799]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM061115, T32GM008799] Funding Source: NIH RePORTER
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.
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