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Expanding the Applicability of the Metal Labeling of Biomolecules by the RIKEN Click Reaction: A Case Study with Gallium‐68 Positron Emission Tomography |
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| Authors: | Yuka Nakamoto Dr. Ambara R. Pradipta Dr. Hidefumi Mukai Maki Zouda Dr. Yasuyoshi Watanabe Dr. Almira Kurbangalieva Dr. Peni Ahmadi Dr. Yoshiyuki Manabe Prof. Dr. Koichi Fukase Prof. Dr. Katsunori Tanaka |
| Affiliation: | 1. Department of Chemistry, Graduate School of Science, Osaka University, Toyonaka, Osaka, Japan;2. Biofunctional Synthetic Chemistry Laboratory, RIKEN Cluster for Pioneering Research, Wako, Saitama, Japan;3. Laboratory for Molecular Delivery and Imaging Technology, RIKEN Center for Biosystems Dynamics Research, Chuo-ku, Kobe, Hyogo, Japan;4. Laboratory for Pathophysiological and Health Science, RIKEN Center for Biosystems Dynamics Research, Chuo-ku, Kobe, Hyogo, Japan;5. Biofunctional Chemistry Laboratory, Butlerov Institute of Chemistry, Kazan Federal University, Kazan, Russia;6. GlycoTargeting Research Laboratory, RIKEN Baton Zone Program, Wako, Saitama, Japan |
| Abstract: | Radiolabeled biomolecules with short half‐life times are of increasing importance for positron emission tomography (PET) imaging studies. Herein, we demonstrate an improved and generalized method for synthesizing a [radiometal]‐unsaturated aldehyde as a lysine‐labeling probe that can be easily conjugated into various biomolecules through the RIKEN click reaction. As a case study, 68Ga‐PET imaging of U87MG xenografted mice is demonstrated by using the 68Ga‐DOTA‐RGDyK peptide, which is selective to αVβ3 integrins. |
| Keywords: | biomolecules click chemistry gallium positron emission tomography radiopharmaceuticals |