前体 microRNA 结合的氨基糖苷类抗生素和抗肿瘤药物作为 Dicer 催化的 microRNA 加工抑制剂。
Pre-microRNA binding aminoglycosides and antitumor drugs as inhibitors of Dicer catalyzed microRNA processing.
机构信息
Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1709-11. doi: 10.1016/j.bmcl.2011.12.103. Epub 2011 Dec 30.
Over-expressions of miRNAs are being increasingly linked with many diseases including different types of cancer. In this study, the role of some known small molecular therapeutics has been investigated for their ability to bind with the pre-miRNA target (hsa-mir-155) and thereby to interfere with the Dicer catalyzed miRNA processing. Potential binding and inhibition effects have been demonstrated by some of these analogs. They can be used as leads for further development of potent small molecular miRNA-antagonists.
miRNAs 的过表达与许多疾病有关，包括不同类型的癌症。在这项研究中，研究了一些已知的小分子治疗药物的作用，以了解它们与 pre-miRNA 靶标（hsa-mir-155）结合的能力，从而干扰 Dicer 催化的 miRNA 加工。这些类似物中的一些已经证明具有潜在的结合和抑制作用。它们可以用作进一步开发有效小分子 miRNA 拮抗剂的先导物。
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