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Covalent stabilization of a small molecule-RNA complex

  作者 Peacock, H; Bachu, R; Beal, PA  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2011年21-17;  页码  5002-5005  
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[摘要]We demonstrate covalent bond formation between an RNA aptamer containing a cysteamine-tethered nucleobase and helix-threading peptides (HTPs) containing alpha-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. (C) 2011 Elsevier Ltd. All rights reserved.

 
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