DNA结合型吡咯-咪唑聚酰胺的相对细胞通透性研究。
Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides.
作者信息
Liu Bo, Kodadek Thomas
机构信息
Department of Internal Medicine, Division of Translational Research, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390, USA.
出版信息
J Med Chem. 2009 Aug 13;52(15):4604-12. doi: 10.1021/jm9002999.
Abstract
Pyrrole-imidazole (Py-Im) polyamides are a group of chemicals that are able to bind specifically to DNA sequences in vitro and in mammalian cells. Using a cell based reporter assay, we investigated the size and linker affects on the cellular permeability of polyamides. We found that the conventional beta-alanine-3,3'-diamino-N-methyldipropylamine (betaDa) linker strongly limited the cellular permeability. We discovered that a short ethylene diamine (Et) linker displayed high cellular permeability. With the improved Et linker, we found that the cellular permeability of polyamides was size-dependent.
摘要
吡咯-咪唑（Py-Im）聚酰胺是一类能够在体外和哺乳动物细胞中与DNA序列特异性结合的化学物质。利用基于细胞的报告基因检测，我们研究了大小和连接体对聚酰胺细胞通透性的影响。我们发现，传统的β-丙氨酸-3,3'-二氨基-N-甲基二丙胺（βDa）连接体严重限制了细胞通透性。我们发现短的乙二胺（Et）连接体具有较高的细胞通透性。使用改进的Et连接体，我们发现聚酰胺的细胞通透性与大小有关。
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