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用于治疗目的的核酸适配体的化学修饰

Chemical Modifications of Nucleic Acid Aptamers for Therapeutic Purposes.

作者信息

Ni Shuaijian, Yao Houzong, Wang Lili, Lu Jun, Jiang Feng, Lu Aiping, Zhang Ge

机构信息

Institute of Precision Medicine and Innovative Drug Discovery, School of Chinese Medicine, Hong Kong Baptist University (HKBU), Hong Kong 999077, China.

Institute for Advancing Translational Medicine in Bone & Joint Diseases, School of Chinese Medicine, Hong Kong Baptist University (HKBU), Hong Kong 999077, China.

出版信息

Int J Mol Sci. 2017 Aug 2;18(8):1683. doi: 10.3390/ijms18081683.

DOI:10.3390/ijms18081683
PMID:28767098
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5578073/
Abstract

Nucleic acid aptamers have minimal immunogenicity, high chemical synthesis production, low cost and high chemical stability when compared with antibodies. However, the susceptibility to nuclease degradation, rapid excretion through renal filtration and insufficient binding affinity hindered their development as drug candidates for therapeutic applications. In this review, we will discuss methods to conquer these challenges and highlight recent developments of chemical modifications and technological advances that may enable early aptamers to be translated into clinical therapeutics.

摘要

与抗体相比，核酸适配体具有最小的免疫原性、高化学合成产量、低成本和高化学稳定性。然而，核酸适配体易受核酸酶降解、通过肾滤过快速排泄以及结合亲和力不足等问题阻碍了它们作为治疗应用候选药物的开发。在本综述中，我们将讨论克服这些挑战的方法，并重点介绍化学修饰的最新进展和技术进步，这些进展可能使早期的适配体转化为临床治疗药物。

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