Department of Nuclear Medicine, Santa Maria Goretti Hospital , Latina, Italy.
Department of Medical and Surgical Sciences and Biotechnology, University of Rome "La Sapienza" , Latina, Italy.
Expert Rev Med Devices. 2020 Aug;17(8):751-758. doi: 10.1080/17434440.2020.1796633. Epub 2020 Jul 27.
aptamers are short artificial, single-strand oligonucleotide sequences (DNA, RNA or modified RNA), capable of binding to biological molecules with high affinity and specificity. Due to their relatively low cost of production and scarce immunogenicity, many efforts have been made to produce aptamers directed against specific molecular targets, such as receptors or transporters overexpressed by malignancies.
the technological approaches for generating aptamers are reviewed. Furthermore, the applications of radiolabeled aptamers for the imaging of several oncological biomarkers through single photon emission computed tomography (SPECT) or positron emission tomography (PET), are covered. Lastly, targeted therapy based on the utilization of aptamers labeled with radionuclides emitting beta particles is discussed, with particular emphasis to the oncological perspectives.
The main limitation of radiolabeled aptamers is represented by their sensitivity to endogenous nuclease, so that several strategies have been developed to increase the stability of these compounds. Although the applications of aptamers are still in a preliminary and pre-clinical phase, it is reasonable to hypothesize that this technology will play a major role for personalized medicine in the next years.
适体是短的人工单链寡核苷酸序列(DNA、RNA 或修饰的 RNA),能够与生物分子高亲和力和特异性结合。由于其生产成本相对较低且免疫原性稀少,因此已经做出许多努力来生产针对特定分子靶标的适体,例如恶性肿瘤过度表达的受体或转运体。
综述了产生适体的技术方法。此外,还介绍了放射性标记适体通过单光子发射计算机断层扫描 (SPECT) 或正电子发射断层扫描 (PET) 对几种肿瘤生物标志物进行成像的应用。最后,讨论了基于放射性核素标记适体的靶向治疗,重点介绍了肿瘤学方面的观点。
放射性标记适体的主要限制在于其对内源核酸酶的敏感性,因此已经开发了几种策略来提高这些化合物的稳定性。尽管适体的应用仍处于初步和临床前阶段,但有理由假设这项技术将在未来几年在个性化医疗中发挥重要作用。