Lee Mun-kyung, Lim Yong-beom
Translational Research Center for Protein Function Control and Department of Materials Science & Engineering, Yonsei University, Seoul 120-749, Republic of Korea.
Translational Research Center for Protein Function Control and Department of Materials Science & Engineering, Yonsei University, Seoul 120-749, Republic of Korea.
Bioorg Med Chem. 2014 Aug 1;22(15):4204-9. doi: 10.1016/j.bmc.2014.05.041. Epub 2014 May 27.
Covalent conjugation of disparate peptide and oligonucleotide biomacromolecular species produces peptide-oligonucleotide conjugates (POCs), which are interesting molecules with great potential for use in diverse bioapplications. However, peptide-oligonucleotide conjugation methods are not well established, and the intracellular delivery efficacy of POCs is debatable. Here, we describe a simple method for the synthesis and purification of POCs. When peptides are carefully designed to have a near-neutral charge state, a relatively hydrophobic polarity, and receptor-targeting ligands, synthesis and purification become highly efficient and straightforward. UV-vis, fluorescence, and circular dichroism studies show that both types of molecules mutually influence each other, changing their optical and conformational characteristics in the context of POCs. The combined effect of peptide design strategy, targeting ligands, and relatively hydrophobic property, enables the efficient cellular delivery of POCs.
将不同的肽和寡核苷酸生物大分子共价缀合可产生肽 - 寡核苷酸缀合物（POC），这些分子很有趣，在多种生物应用中具有巨大的应用潜力。然而，肽 - 寡核苷酸缀合方法尚未完全确立，POC的细胞内递送效果也存在争议。在此，我们描述了一种合成和纯化POC的简单方法。当肽经过精心设计，具有接近中性的电荷状态、相对疏水的极性和受体靶向配体时，合成和纯化变得高效且直接。紫外可见光谱、荧光光谱和圆二色性研究表明，两种类型的分子相互影响，在POC的背景下改变它们的光学和构象特征。肽设计策略、靶向配体和相对疏水性质的综合作用，使得POC能够高效地递送至细胞。
