Department of Chemistry, Graduate School of Science, Kyoto University, Kitashirakawa oiwakecho, Kyoto 606-8502, Japan.
Chembiochem. 2012 Oct 15;13(15):2170-85. doi: 10.1002/cbic.201200451. Epub 2012 Sep 28.
Recently, the versatility of N-methylpyrrole (Py)-N-methylimidazole (Im) polyamide conjugates, which have been developed from the DNA-binding antibiotics distamycin A and netropsin, has been shown. These synthetic small molecules can permeate cells to bind with duplex DNA in a sequence-specific manner, and hence can influence gene expression in vivo. Accordingly, several reports demonstrating the sequence specificity and biological activity of Py-Im polyamides have accumulated. However, the benefits of Py-Im polyamides, in particular those conjugated with fluorophores, has been overlooked. Moreover, clear directions for the employment of these attractive artificial small molecules have not yet been shown. Here, we present a detailed overview of the current and prospective applications of Py-Im polyamide-fluorophore conjugates, including sequence-specific recognition with fluorescence emission properties, and their potential roles in biological imaging.
最近，已经证明了 N-甲基吡咯（Py）-N-甲基咪唑（Im）聚酰胺缀合物的多功能性，这些缀合物是从 DNA 结合抗生素放线菌素 D 和 netropsin 发展而来的。这些合成的小分子可以穿透细胞，以序列特异性的方式与双链 DNA 结合，因此可以在体内影响基因表达。因此，已经积累了几篇证明 Py-Im 聚酰胺的序列特异性和生物活性的报告。然而，Py-Im 聚酰胺的好处，特别是那些与荧光团缀合的聚酰胺，一直被忽视。此外，这些有吸引力的人工小分子的应用还没有明确的方向。在这里，我们详细介绍了 Py-Im 聚酰胺-荧光团缀合物的当前和潜在应用，包括与荧光发射特性的序列特异性识别，以及它们在生物成像中的潜在作用。
