Aluminum fluoride-18-labelled indocyanine green as a potential PET imaging agent for hepatic function reserve

Chen, Kuang; Zhang, Xiaojun; Wang, Fei; Wu, Yitian; Zhou, Haoxi; Zhang, Ying; Zou, Wei; Zhang, Jinming; Liu, Rong

doi:10.1007/s10967-022-08359-1

Cited by 1 publication

(3 citation statements)

References 17 publications

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“…The Log P value of [ 18 F]AlF-RSM was determined to be −0.90 ± 0.01, which was more hydrophilic than [ 18 F]SF-AAN-M (0.11 ± 0.04), owing to the RESCA moiety. [ 18 F]AlF-RESCA-ICG , a recently reported small-molecule radiotracer for assessing the hepatic function, was radio-synthesized with a radiochemical yield (RCY) of 28.9 ± 1.5%. van der Veen et al also reported a tracer [ 18 F]AlF-RESCA-IL2 for T cell imaging with an RCY of 2.4 ± 1.6% .…”

Section: Resultsmentioning

confidence: 99%

“…Compounds RSM and [ 19 F]AlF-RSM were synthesized according to the literature (Figures S2 and S3). 27,35 All chemical characterizations of compounds were determined by HPLC and ESI-MS (Figures S4−S13 QMA cartridge. [ 18 F]F − was eluted from the QMA cartridge with 0.3 mL of 0.9% saline solution.…”

Section: Synthesis Of Nonradioactive Rsm and [ 19 F]alf-rsmmentioning

confidence: 99%

“…Compounds RSM and [ 19 F]AlF-RSM were synthesized according to the literature (Figures S2 and S3). , All chemical characterizations of compounds were determined by HPLC and ESI-MS (Figures S4–S13).…”

Section: Experimental Sectionsmentioning

confidence: 99%

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Legumain-Triggered Macrocyclization of Radiofluorinated Tracer for Enhanced PET Imaging

Gao,

Wang,

Yang

et al. 2024

Bioconjugate Chem.

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Enhancing the accumulation and retention of small-molecule probes in tumors is an important way to achieve accurate cancer diagnosis and therapy. Enzyme-stimulated macrocyclization of small molecules possesses great potential for enhanced positron emission tomography (PET) imaging of tumors. Herein, we reported an 18 F-labeled radiotracer [ 18 F]AlF-RSM for legumain detection in vivo. The tracer was prepared by a one-step aluminum-fluoride-restrained complexing agent ([ 18 F]AlF-RESCA) method with high radiochemical yield (RCY) (88.35 ± 3.93%) and radiochemical purity (RCP) (>95%). More notably, the tracer can be transformed into a hydrophobic macrocyclic molecule under the joint action of legumain and reductant. Simultaneously, the tracer could target legumain-positive tumors and enhance accumulation and retention in tumors, resulting in the amplification of PET imaging signals. The enhancement of radioactivity enables PET imaging of legumain activity with high specificity. We envision that, by combining this highly efficient 18 F-labeled strategy with our intramolecular macrocyclization reaction, a range of radiofluorinated tracers can be designed for tumor PET imaging and early cancer diagnosis in the future.

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Section: Resultsmentioning

confidence: 99%

Section: Synthesis Of Nonradioactive Rsm and [ 19 F]alf-rsmmentioning

confidence: 99%