作　　者： (堵玉林）; (梁静）;

机构地区： 中国矿业大学化工学院,徐州221116

出　　处： 《化学通报》 2017年第9期809-818,862,共11页

摘　　要： 传统的抗肿瘤药物大多不具有选择性,在临床治疗中产生了严重的毒副作用。核酸适配体是一种小分子核酸,能够与靶标高亲和性、高特异性地结合。选择与癌症发生发展过程密切相关的生物标记物为靶标进行SELEX过程筛选出的核酸适配体自身可作为药物,也可与药物、siRNA、纳米粒等结合构成靶向给药体系,该体系能靶向作用于特定的肿瘤细胞,降低对正常细胞的毒性,用药量显著降低,药效提高。本文综述了近年来核酸适配体直接作为抗肿瘤药物、药物载体、siRNA载体以及作为纳米材料靶向剂构成多元复合靶向给药体系在肿瘤靶向治疗领域的研究进展。 Traditional anti-tumor drugs can cause serious side effects in clinical treatment due to their nonspecific toxicity. Aptamers are a class of small nucleic acid ligands that have high affinity and specificity for their targets. Well-characterized biomarkers,especially those closely related to the development of cancer,can be used as targets for aptamer selection via the SELEX method. The newly obtained aptamers may be able to act as drugs themselves,or conjugate with other chemical drugs,siRNA,and nanoparticles to generate targeted drug delivery systems which can target specific tumor cells,thus minimizing the toxicity to normal cells,reducing the dose needed for treatment and enhancing therapeutic efficacy. In this review,we summarize the current advances in the application of aptamers in tumor targeted therapy with aptamers as anti-tumor drugs,as drug carriers,as RNA-based therapeutic carriers or as targeted ligands for conjugates with nanoparticles.

关 键 词： 核酸适配体 抗肿瘤药物 靶向治疗 纳米材料