Department of Bioengineering, Graduate School of Engineering, Osaka City University, Sumiyoshi-ku, Osaka, Japan.
FEBS Lett. 2012 May 21;586(10):1529-32. doi: 10.1016/j.febslet.2012.04.013. Epub 2012 Apr 20.
Many miRNA inhibitors have been developed and they are chemically modified oligonucleotides such as 2?-O-methylated RNA and locked nucleic acid (LNA). Unmodified DNA was not yet reported as a miRNA inhibitor because of the low affinity of DNA/miRNA compared to mRNA/miRNA. We designed a structured unmodified DNA that significantly inhibits miRNA function. The clue structure for activity is the miRNA binding site between double stranded regions which is responsible for the miRNA inhibitory activity and tight binding to miRNA. We developed the miRNA inhibitor constructed with unmodified DNA, and named it LidNA, DNA that puts a lid on miRNA function.
许多 miRNA 抑制剂已经被开发出来,它们是经过化学修饰的寡核苷酸,如 2'-O-甲基化 RNA 和锁核酸 (LNA)。由于 DNA 与 miRNA 的亲和力低于 mRNA 与 miRNA 的亲和力,因此未经修饰的 DNA 尚未被报道为 miRNA 抑制剂。我们设计了一种结构未修饰的 DNA,它能显著抑制 miRNA 的功能。活性的关键结构是双链区域之间的 miRNA 结合位点,该位点负责 miRNA 的抑制活性和与 miRNA 的紧密结合。我们开发了一种由未修饰 DNA 构建的 miRNA 抑制剂,并将其命名为 LidNA,即能封闭 miRNA 功能的 DNA。