Department of Laboratory Medicine, Karolinska Institutet, Clinical Research Center, Karolinska University Hospital Huddinge, Hälsovägen 7, 141 83 Huddinge, Sweden.
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5635-8. doi: 10.1016/j.bmcl.2012.06.103. Epub 2012 Jul 7.
Here we report a novel class of peptides-d-diaminopropionic acids (Dap)-for gene delivery. These peptides have attractive properties for gene delivery, and the advantage that they can be easily manipulated in relation to their composition, abiding with tailored-design. We characterized the toxicological and biophysical properties of DNA particles resulting from the interaction of the nucleic acid with a series of Dap(8) peptides conjugated to different alkyl groups. These peptides formed small and homogenous DNA particle populations that protected against DNase I degradation at non-toxic concentrations. However, despite the similarity between these peptides and others that are arginine-rich, and efficient vectors, functional studies suggest the need for additional modifications in the carriers to improve their DNA delivery efficiency. Taken together, these studies underscore the relevance of the overall structure of the carrier and the complexity of designing from scratch a carrier.
在这里，我们报告了一类新型的肽——二氨基丙酸（Dap），用于基因传递。这些肽具有吸引人的基因传递特性，并且具有可以根据其组成进行轻松操作的优势，符合定制设计的要求。我们研究了与一系列与不同烷基基团缀合的 Dap(8)肽相互作用而产生的 DNA 颗粒的毒理学和生物物理特性。这些肽形成了小而均匀的 DNA 颗粒群体，在非毒性浓度下能防止 DNA 酶 I 的降解。然而，尽管这些肽与其他富含精氨酸的有效载体相似，但功能研究表明，需要对载体进行额外的修饰，以提高其 DNA 传递效率。总的来说，这些研究强调了载体整体结构的重要性，以及从头设计载体的复杂性。
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