Radiolabeling of peptides, nanobodies, and aptamers for positron emission tomography (PET)

Authors

• D Kiesewetter
• L Lang
• J Gonzalez-Guzman

Abstract

Our NIBIB core facility has a mission to provide state of the art positron emission tomography imaging in small animals. Our equipment includes a Mediso nanoScan PET/CT instrument to provide high quality, quantitative images of radioisotope distribution in mice or rats. In addition, we have a radiochemistry facility to synthesize Ga-68, Cu-64 and F-18 labeled radiotracers. We now have available fluorine-18 labeled prosthetic groups that can be attached to peptides, nanobodies, and aptamers. Using copper-mediated radiofluorination of aryl boronates, we have prepared N-hydroxysuccinimidyl [18F]fluorobenzoate for attachment to lysine residues; 1-(3-(4-(4-[18F]fluorobenzyl)piperazin-1-yl)-3-oxopropyl)-1H-pyrrole-2,5-dione (a maleimide) for attachment to free cysteine thiol residues; and 2-azido-1(4-(4-[18F]fluorobenzylpiperazin-1-yl)ethan-1-one for attachment to alkyne residues using copper catalyzed “click” chemistry. The preparation methods for the various compounds utilize the same automated radiosynthesis system with only slight variations in purification conditions. These compounds can be conjugated to appropriate biomolecules and the resulting product used for PET/CT imaging.

Scientific Focus Area: Research Support Services

This page was last updated on Tuesday, August 6, 2024