寡聚酰胺化学与生物学研究进展

Advances in the chemical and biological studies of polyamides

含有吡咯和咪唑的寡聚酰胺是一类人工合成的小分子化合物,其分子形状与DNA小沟的曲率相吻合,能高亲合力和特异性地与DNA小沟中特定序列进行识别并结合,从而起到调控基因表达的作用。寡聚酰胺易透过细胞膜、无细胞毒性、结构稳定和不易降解,是一类很有前途的基因调控工具。本文从寡聚酰胺配对规则、对DNA序列的选择性与结合力、合成方法、透膜吸收、基因调控和动物体内实验等方面的研究进展进行综述,并讨论其在研究中面临的问题,为寡聚酰胺的研究提供参考。

Polyamides, containing N-methylpyrrole （Py） and N-methyl-imidazole （Im） amino acids, are synthetic oligomers programmed to read the DNA double helix in the minor groove with high affinities and sequence specificities resulting in modulation of gene expression. They are cell permeable, stable and have no cytotoxicity, which provide a promising tool of gene regulation. We describe here recent advances in the field of DNA binding polyamides, including pairing rules, specifities and affinities to DNA, synthesis methods, cellular and nuclear uptake properties, gene regulation and effectiveness in vivo. The potential problems and difficulties in future research are also discussed.