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对适体药物偶联物(ApDCs)的基本了解。

A basic insight into aptamer-drug conjugates (ApDCs).

机构信息

Molecular Science and Biomedicine Laboratory, State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, College of Life Sciences, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha, Hunan 410082, China.

Institute of Molecular Medicine, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai Jiao Tong University, College of Chemistry and Chemical Engineering, Shanghai 200240, China.

出版信息

Biomaterials. 2018 Nov;182:216-226. doi: 10.1016/j.biomaterials.2018.08.021. Epub 2018 Aug 8.

DOI:10.1016/j.biomaterials.2018.08.021
PMID:30138784
Abstract

Aptamers are often compared with antibodies since both types of molecules function as targeting ligands for specific cancer cell recognition. However, aptamers offer several advantages, including small size, facile chemical modification, high chemical stability, low immunogenicity, rapid tissue penetration, and engineering simplicity. Despite these advantages, several crucial factors have delayed their clinical translation, such as concerns over inherent physicochemical stability and safety. Meanwhile, steps have been taken to make aptamer-drug conjugates, or ApDCs, a clinically practical tool. In this review, we highlight the development of ApDCs and discuss how researchers are solving some problems associated with their clinical application for targeted therapy.

摘要

适体常被比作抗体,因为这两种分子都作为靶向配体,用于识别特定的癌细胞。然而,适体具有一些优势,包括体积小、易于化学修饰、化学稳定性高、免疫原性低、组织穿透迅速以及易于工程化。尽管具有这些优势,但一些关键因素仍阻碍了其临床转化,如对固有理化稳定性和安全性的担忧。与此同时,人们已经采取措施,使适体-药物偶联物(ApDC)成为一种临床实用工具。在这篇综述中,我们重点介绍了 ApDC 的发展,并讨论了研究人员如何解决与靶向治疗相关的一些临床应用问题。

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