Molecular Imaging for Radiolabeling a PSMA-Targeted Long Circulating Peptide as a Theranostic Agent in Mice Bearing a Human Prostate Tumor

Cyanopyridoimidazole/1,2-Aminothiol Click Reaction: A Novel Bioorthogonal Reaction for Synthesis of Radiotracers

“…With 14 in hand, we next investigated the feasibility of the application of 14 as a prosthetic group in two-step labeling by testing whether its cyano group could tolerate the labeling conditions. Under conventional labeling conditions (0.1 M NaOAc buffer, pH 4.5, 90 °C, 15 min), we labeled 14 with nonradioactive gallium ([ nat Ga]Ga) to give [ nat Ga]Ga- 14 in a quantitative yield (Figure S6). Further condensation of [ nat Ga]Ga- 14 and l -cysteine generated the clicked product ( S15 ) exclusively, demonstrating that the CPI remained functional.…”