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Pharmaceuticals 2018, 11(4), 106; https://doi.org/10.3390/ph11040106

Radiolabeling of Nucleic Acid Aptamers for Highly Sensitive Disease-Specific Molecular Imaging

1
Department of Nuclear Medicine, School of Medicine, Rajaie Cardiovascular, Medical and Research Center & Department of Medicinal Chemistry, School of Pharmacy-International Campus, Iran University of Medical Sciences, Tehran 1449614535, Iran
2
Centre for Comparative Genomics, Murdoch University, Perth 6150, Australia
3
Perron Institute for Neurological and Translational Science, Perth 6009, Australia
*
Author to whom correspondence should be addressed.
Received: 22 August 2018 / Revised: 6 October 2018 / Accepted: 10 October 2018 / Published: 15 October 2018
(This article belongs to the Special Issue Aptamer-Based Diagnostics and Therapeutics)
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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. View Full-Text
Keywords: aptamers; aptamer-targeted imaging; molecular imaging; aptamer-radiolabeling aptamers; aptamer-targeted imaging; molecular imaging; aptamer-radiolabeling
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Hassanzadeh, L.; Chen, S.; Veedu, R.N. Radiolabeling of Nucleic Acid Aptamers for Highly Sensitive Disease-Specific Molecular Imaging. Pharmaceuticals 2018, 11, 106.

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