The interdiscipline rendezvous of aptamers and radionuclides: Advances, challenges and prospects

Aptamers have emerged as versatile tools in biomedical applications spanning biosensing, medical imaging, and therapeutic interventions. Radionuclides as the therapeutic and diagnostic agents, with simple molecular structures and good safety profile, represent one of the most mature theranostics technologies. Under the overarching trend of interdisciplinary and cross-integrated research, radionuclide-labeled aptamers have garnered significant scientific interest as dual-functional agents offering precise diagnostic and therapeutic potential. In this review, the latest progresses of aptamer selection and the different modification strategies for aptamer performance enhancement for in vivo applications are summarized. Radionuclides, strategies for aptamer radiolabeling, and their applications in disease diagnosis, treatment, and pharmacokinetic studies are emphasized. Although there are still obstacles of radiolabeled aptamers for clinical translation, we envision that more precise and efficient molecular drugs and tools will be developed in the near future against the backdrop of cross-collaboration between the two major fields of nucleic acid aptamers and radionuclides.