Abstract：
In this work, we investigate the compaction activity of a sequential alpha,epsilon-peptide composed of l-lysines towards two RNA targets, in view of its possible pharmaceutical application in RNA-targeting and RNA delivery. The basic oligolysine, object of the present study, proved not only to be efficient in compacting the single-stranded polyA RNA, but also to strongly interact with the polyA·polyU complex, as evidenced by CD-binding and UV-melting experiments. In particular, the marked differences in the CD spectra of the RNA targets upon addition of the peptide, as well as the different UV melting behaviour for the polyA·polyU complex in the presence and absence of the peptide, sustain the hypothesis of a strong RNA compaction capacity of the alpha,epsilon-oligolysine. Finally, by using HPLC analysis, we found a good resistance of the peptide against the lytic action of human serum, an important requirement in view of in vitro/in vivo biological assays.
摘要：
在这项工作中,我们研究了连续α的压实活性，由l-赖氨酸组成的ε-肽对两个RNA靶标，鉴于其在RNA靶向和RNA递送中可能的药物应用。基本的寡赖氨酸，本研究的对象，被证明不仅可以有效地压缩单链polyARNA，而且还与polyA·polyU复合物强烈相互作用，如CD结合和UV熔化实验所证明的。特别是,添加肽后，RNA靶标的CD光谱存在明显差异，以及在存在和不存在肽的情况下，polyA·polyU复合物的不同紫外线熔化行为，支持α的强RNA压缩能力的假设，ε-寡赖氨酸。最后,通过使用HPLC分析，我们发现该肽对人血清的裂解作用具有良好的抗性，鉴于体外/体内生物测定的重要要求。
