UMR 892 INSERM, 6299 CNRS, Nantes, France.
Epigenomics. 2014 Jun;6(3):267-75. doi: 10.2217/epi.14.18.
DNA methylation is a fundamental biologic process of genomes and is a candidate for pharmacological manipulation that might have important therapeutic advantages. Thus, DNA methyltransferases (DNMTs) appear to be ideal targets for drug intervention.
MATERIALS & METHODS: To develop a new generation of DNMT inhibitor, we analyzed the ability of peptides to selectively inhibit certain DNMT1-incuding complexes.
Our study demonstrates that the disruption of DNMT1/CFP1-including complexes increases the efficiency of chemotherapeutic treatment on established tumors in mice.
Our data opens a promising and innovative alternative to the development of DNMT inhibitors.
DNA 甲基化是基因组的基本生物学过程，是药物干预的候选对象，可能具有重要的治疗优势。因此，DNA 甲基转移酶（DNMTs）似乎是药物干预的理想靶点。
为了开发新一代的 DNMT 抑制剂，我们分析了肽选择性抑制某些包含 DNMT1 的复合物的能力。
我们的研究表明，破坏包含 DNMT1/CCCTC 结合因子 1（CFP1）的复合物可提高化疗药物在小鼠已建立肿瘤中的治疗效果。
我们的数据为开发 DNMT 抑制剂提供了一种有前景的创新选择。
Zotero 插件