Department of Chemistry, University of California, One Shields Ave, Davis, CA 95616, United States.
Bioorg Med Chem Lett. 2011 Sep 1;21(17):5002-5. doi: 10.1016/j.bmcl.2011.04.136. Epub 2011 May 5.
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.
我们证明了含有半胱胺键合碱基的 RNA 适体与含有α-溴乙酰胺 N-末端的螺旋穿入肽(HTP)之间的共价键形成。该反应产率高,并被与适体序列互补的 DNA 链 Watson-Crick 抑制,表明共价反应取决于折叠适体中存在的高亲和力 HTP 结合位点。这些结果对于未来的 HTP-RNA 复合物结构研究以及通过共价键合策略发现新的高亲和力类似物的方法非常重要。