Radiolabeling of functional oligonucleotides for molecular imaging

Dunfang Liu; Qian Xia; Ding Ding; Weihong Tan

doi:10.3389/fbioe.2022.986412

Radiolabeling of functional oligonucleotides for molecular imaging

Front Bioeng Biotechnol. 2022 Aug 19:10:986412. doi: 10.3389/fbioe.2022.986412. eCollection 2022.

Authors

Dunfang Liu^{1

2}, Qian Xia^{1

2}, Ding Ding¹, Weihong Tan^{1

3

4}

Affiliations

¹ Institute of Molecular Medicine (IMM), Renji Hospital, State Key Laboratory of Oncogenes and Related Genes, Shanghai Jiao Tong University School of Medicine and College of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, China.
² Department of Nuclear Medicine, Institute of Clinical Nuclear Medicine, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
³ The Cancer Hospital of the University of Chinese Academy of Sciences (Zhejiang Cancer Hospital), Hangzhou Institute of Medicine (HIM), Chinese Academy of Sciences, Hangzhou, Zhejiang, China.
⁴ Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, Hunan, China.

Abstract

Molecular imaging has greatly advanced basic biology and translational medicine through visualization and quantification of molecular events in a cellular context and living organisms. Nuclear medicine, including positron emission tomography (PET) and single-photon emission tomography (SPECT), is one of the most representative molecular imaging modalities which is widely used in clinical theranostics. Recently, numerous molecular imaging agents have been developed to improve the quality and expand the applicable diseases of molecular imaging. Based on the choice of specific imaging agents, molecular imaging is capable of studying tumor biological activities, detecting tumor metastasis, and imaging Alzheimer's disease-related amyloid proteins. Among these imaging agents, functional oligonucleotides-based imaging probes are becoming increasingly important due to their unique features. Antisense oligonucleotides, small interfering RNA, and aptamers are privileged molecular tools in precision medicine for cancer diagnosis and treatment. These chemically synthesized oligonucleotides without batch-to-batch variations are flexible to incorporate with other molecules without affecting their functionalities. Therefore, through the combination of oligonucleotides with radioisotopes, a series of molecular imaging agents were developed in the past decades to achieve highly sensitive and accurate biomedical imaging modalities for clinical theranostic. Due to the nature of oligonucleotides, the strategies of oligonucleotide radiolabeling are different from conventional small molecular tracers, and the radiolabeling strategy with rational design is highly correlated to the imaging quality. In this review, we summarize recent advancements in functional oligonucleotide radiolabeling strategies and respective molecular imaging applications. Meanwhile, challenges and future development insights of functional oligonucleotide-based radiopharmaceuticals are discussed in the end.

Keywords: functional oligonucleotides; molecular imaging; precision medecine; radiolabeling; radiopharmaceutical.

Publication types

Review