Improved Anti-Prion Nucleic Acid Aptamers by Incorporation of Chemical Modifications
Improved Anti-Prion Nucleic Acid Aptamers by Incorporation of Chemical Modifications
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DOI：
10.1089/nat.2020.0899
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发表时间：
2020-09-29
影响因子：
4
通讯作者：
Pagano, Bruno
中科院分区：
文献类型：
--
作者：
Amato, Jussara;Mashima, Tsukasa;Pagano, Bruno
核酸适体是阻断朊病毒疾病的标志性事件，即朊病毒蛋白（PrP）转化为异常形式的创新和有前途的候选体；然而，它们需要化学修饰才能获得有效的治疗活性。本文报道了一个靶向细胞PrP的化学修饰g -四重体形成适体的小文库的开发和生物物理特性，并评估了它们的抗朊病毒活性。结果表明，通过直接修饰可以增强抗朊病毒适配体的性能。
Nucleic acid aptamers are innovative and promising candidates to block the hallmark event in the prion diseases, that is the conversion of prion protein (PrP) into an abnormal form; however, they need chemical modifications for effective therapeutic activity. This communication reports on the development and biophysical characterization of a small library of chemically modified G-quadruplex-forming aptamers targeting the cellular PrP and the evaluation of their anti-prion activity. The results show the possibility of enhancing anti-prion aptamer properties through straightforward modifications.