Abstract

Aptamers are short single-stranded DNA or RNA oligonucleotide ligand molecules with a unique three-dimensional shape, capable of binding to a defined molecular target with high affinity and specificity. Since their discovery, aptamers have been developed for various applications, including molecular imaging, particularly nuclear imaging that holds the highest potential for the clinical translation of aptamer-based molecular imaging probes. Their easy laboratory production without any batch-to-batch variations, their high stability, their small size with no immunogenicity and toxicity, and their flexibility to incorporate various functionalities without compromising the target binding affinity and specificity make aptamers an attractive class of targeted-imaging agents. Aptamer technology has been utilized in nuclear medicine imaging techniques, such as single photon emission computed tomography (SPECT) and positron emission tomography (PET), as highly sensitive and accurate biomedical imaging modalities towards clinical diagnostic applications. However, for aptamer-targeted PET and SPECT imaging, conjugation of appropriate radionuclides to aptamers is crucial. This review summarizes various strategies to link the radionuclides to chemically modified aptamers to accomplish aptamer-targeted PET and SPECT imaging.

Highlights

  • Molecular imaging technologies employ labeled molecules to explore biological targets in living subjects for disease detection and monitoring treatment progress in real time

  • We focus on various methods of radiolabeling that have have performed aptamers potential approaches to producing diagnostic tracers been been performed usingusing aptamers and and otherother potential approaches to producing diagnostic tracers in in imaging techniques

  • In 2016, Fletcher et al reported the attachment of an oligonucleotide aptamer with Hyperbranched Polymers (HBPs) targeting VEGF (VEGF), which are upregulated in triple‐negative breast cancer

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Summary

Introduction

Molecular imaging technologies employ labeled molecules to explore biological targets in living subjects for disease detection and monitoring treatment progress in real time. Pharmaceutics 2018, FOR PEER REVIEW hydrophobic effects, Vander Waals forces, and so on, enable them to bind the target binding domain (aptatope) [6]. Aptamers are able to bind different types of targets, such as small ions like Zn2+, large large like proteins, whole cells, bacteria, viruses [7,8,9,10]. D or L amino acids that make them highly specific urea against a guanidine group, and D or L amino acids that make them highly specific compounds compounds [11,12,13,14] Their high specificity, solid phase chemical synthesis, andsize small fortissue high [11,12,13,14].

Improving
SPECT and PET Imaging Techniques
Radiolabeling of Ligands for SPECT Imaging
Indirect
Conjugation
Radiolabeling
F Radiolabeling
Synthesis
10. Conjugation
Silicon‐Based
18 F were
18 F–SFB using was modified to have a
Hybridization-Based 18 F-Radiolabeling of Aptamers
64 Cu-Radiolabeling
64 Cu can be achieved under
Desferrioxamine B Chelating Agent
Zirconium-89 Labeling
17. Conjugation
68 Gaconjugated reportedwere labeling of at uMUC-1
20. Thiol–maleimide
Findings
Conclusions and Future Prospects
Full Text
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