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Article Abstract
Protein-based F-PET tracers offer new possibilities in early disease detection and personalized medicine. Their development relies heavily on the availability and effectiveness of F-prosthetic groups. We prepared and evaluated a novel arginine-selective prosthetic group, 4-[F]fluorophenylglyoxal ([F]FPG). [F]FPG was radiosynthesized by a one-pot, two-step procedure with a non-decay-corrected (n.d.c.) isolated radiochemical yield (RCY) of 41 ± 8% ( = 10). [F]FPG constitutes a generic tool for F-labeling of various proteins, including human serum albumin (HSA), ubiquitin, interleukin-2, and interleukin-4 in ∼30-60% n.d.c. isolated RCYs. [F]FPG conjugation with arginine residues is highly selective, even in the presence of a large excess of lysine, cysteine, and histidine. [F]FPG protein conjugates are able to preserve the binding affinity of the native proteins while also demonstrating excellent stability. The [F]FPG-HSA conjugate has prolonged blood retention, which can be applied as a potential blood pool PET imaging agent. Thus, [F]FPG is an arginine-selective bioconjugation reagent that can be effectively used for the development of F-labeled protein radiopharmaceuticals.
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| http://dx.doi.org/10.1021/acs.jmedchem.4c00154 | DOI Listing |
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Article Synopsis
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- This tool is good at connecting to a specific part of proteins, called arginine, while ignoring other parts, making it very useful.
- The new protein markers stay stable in the body and can be used for better medical imaging, which might help doctors see how diseases are affecting the blood.
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