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Nucleic Acid Aptamers Targeting Epigenetic Regulators: An Innovative Therapeutic Option

机译:靶向表观遗传调节剂的核酸适体:一种创新的治疗选择

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摘要

Epigenetic mechanisms include DNA methylation, posttranslational modifications of histones, chromatin remodeling factors, and post transcriptional gene regulation by noncoding RNAs. All together, these processes regulate gene expression by changing chromatin organization and DNA accessibility. Targeting enzymatic regulators responsible for DNA and chromatin modifications hold promise for modulating the transcriptional regulation of genes that are involved in cancer, as well as in chronic noncommunicable metabolic diseases like obesity, diabetes, and cardiovascular diseases. Increasingly studies are emerging, leading to the identification of specific and effective molecules targeting epigenetic pathways involved in disease onset. In this regard, RNA interference, which uses small RNAs to reduce gene expression and nucleic acid aptamers are arising as very promising candidates in therapeutic approach. Common to all these strategies is the imperative challenge of specificity. In this regard, nucleic acid aptamers have emerged as an attractive class of carrier molecules due to their ability to bind with high affinity to specific ligands, their high chemical flexibility as well as tissue penetration capability. In this review, we will focus on the recent progress in the field of aptamers used as targeting moieties able to recognize and revert epigenetics marks involved in diseases onset.
机译:表观遗传机制包括DNA甲基化,组蛋白的翻译后修饰,染色质重塑因子以及非编码RNA的转录后基因调控。总之,这些过程通过改变染色质的组织和DNA的可及性来调节基因的表达。靶向负责DNA和染色质修饰的酶促调节剂有望调节与癌症以及肥胖,糖尿病和心血管疾病等慢性非传染性代谢疾病有关的基因的转录调控。越来越多的研究正在涌现,从而导致确定靶向与疾病发作有关的表观遗传途径的特异性和有效分子。在这方面,使用小RNA减少基因表达和核酸适体的RNA干扰已成为治疗方法中非常有前途的候选对象。所有这些策略的共同点是特定性的迫切挑战。在这方面,核酸适体由于其与特定配体的高亲和力结合的能力,其高化学柔韧性以及组织穿透能力而已成为一类有吸引力的载体分子。在这篇综述中,我们将集中在适体作为靶向部分的最新进展,所述适体作为能够识别和逆转涉及疾病发作的表观遗传学标记的部分。

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