Developing native peptide-based radiotracers for PD-L1 PET imaging and improving imaging contrast by pegylation

Herein, a PD-L1 targeted native peptide was developed for PET imaging. 18F and 64Cu were utilized to label the peptide. To improve the pharmacokinetics and biodistribution of the tracers, the peptide was further pegylated to form star-like tetramers. Consequently, four tracers were synthesized with...

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Bibliographic Details
Published inChemical communications (Cambridge, England) Vol. 55; no. 29; pp. 4162 - 4165
Main Authors Hu, Kuan, Kuan, Hu, Hanyu, Masayuki, Masayuki, Hanyu, Xie, Lin, Zhang, Yiding, Nagatsu, Kotaro, Kotaro, Nagatsu, Suzuki, Hisashi, Hisashi, Suzuki, Zhang, Ming-Rong
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 04.04.2019
Subjects
Imaging
In vivo methods and tests
Peptides
Pharmacology
Positron emission
Radioactive tracers
Radiochemistry
Tomography
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Summary:Herein, a PD-L1 targeted native peptide was developed for PET imaging. 18F and 64Cu were utilized to label the peptide. To improve the pharmacokinetics and biodistribution of the tracers, the peptide was further pegylated to form star-like tetramers. Consequently, four tracers were synthesized with acceptable radiochemical characteristics and their in vivo pharmacokinetics and PD-L1 imaging capability were systematically evaluated. This proof-of-principle study may provide new possibilities for PD-L1 PET imaging in cancers.
ISSN:1359-7345
1364-548X
DOI:10.1039/c9cc00445a