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针对酪氨酸激酶受体的寡核苷酸适体:在抗癌应用方面的前景。

Oligonucleotide aptamers against tyrosine kinase receptors: Prospect for anticancer applications.

机构信息

Consiglio Nazionale delle Ricerche, Istituto per l'Endocrinologia e l'Oncologia Sperimentale "G. Salvatore" (IEOS), Via S. Pansini 5, 80131 Naples, Italy.

Consiglio Nazionale delle Ricerche, Istituto per l'Endocrinologia e l'Oncologia Sperimentale "G. Salvatore" (IEOS), Via S. Pansini 5, 80131 Naples, Italy.

出版信息

Biochim Biophys Acta Rev Cancer. 2018 Apr;1869(2):263-277. doi: 10.1016/j.bbcan.2018.03.003. Epub 2018 Mar 21.

Abstract

Transmembrane receptor tyrosine kinases (RTKs) play crucial roles in cancer cell proliferation, survival, migration and differentiation. Area of intense research is searching for effective anticancer therapies targeting these receptors and, to date, several monoclonal antibodies and small-molecule tyrosine kinase inhibitors have entered the clinic. However, some of these drugs show limited efficacy and give rise to acquired resistance. Emerging highly selective compounds for anticancer therapy are oligonucleotide aptamers that interact with their targets by recognizing a specific three-dimensional structure. Because of their nucleic acid nature, the rational design of advanced strategies to manipulate aptamers for both diagnostic and therapeutic applications is greatly simplified over antibodies. In this manuscript, we will provide a comprehensive overview of oligonucleotide aptamers as next generation strategies to efficiently target RTKs in human cancers.

摘要

跨膜受体酪氨酸激酶 (RTKs) 在癌细胞的增殖、存活、迁移和分化中发挥着关键作用。目前,人们正在积极研究针对这些受体的有效抗癌疗法,已有几种单克隆抗体和小分子酪氨酸激酶抑制剂进入临床应用。然而,其中一些药物的疗效有限,并产生获得性耐药性。新兴的高度选择性抗癌治疗化合物是寡核苷酸适体,它们通过识别特定的三维结构与靶点相互作用。由于其核酸性质,与抗体相比,设计用于诊断和治疗应用的先进策略来操纵适体的合理性大大简化。在本文中,我们将全面概述作为下一代策略的寡核苷酸适体,以有效地针对人类癌症中的 RTKs。

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