Abstract
We demonstrate covalent bond formation between an RNA aptamer containing a cysteamine-tethered nucleobase and helix-threading peptides (HTPs) containing α-bromoacetamide N-termini. The reaction is high yielding and inhibited by a DNA strand Watson-Crick complementary to the aptamer sequence indicating covalent reaction is dependent on the high affinity HTP-binding site present in the folded aptamer. These results are important for future structural studies of HTP-RNA complexes and methods for the discovery of new high affinity analogs via covalent tethering strategies.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 5002-5005 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 21 |
| Issue number | 17 |
| DOIs | |
| State | Published - Sep 1 2011 |
Keywords
- Aptamer
- Covalent tethering
- Helix-threading peptide
- Nucleoside analog
- Templated reaction
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
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Cite this
Peacock, H., Bachu, R., & Beal, P. A. (2011). Covalent stabilization of a small molecule-RNA complex. Bioorganic and Medicinal Chemistry Letters, 21(17), 5002-5005. https://doi.org/10.1016/j.bmcl.2011.04.136