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Imaging Protein Synthesis

Imaging Protein Synthesis

Target: rate of protein synthesis

PET radiotracer candidates: [11C]PURO and [18F]FEPURO

Besides two main research themes of neurodegeneration and CNS receptor imaging, we are also interested in other hallmarks of disease, such as rate of protein synthesis. Imaging protein synthesis in vivo using PET is commonly done using amino acid based radiotracers such as [11C]LEU or [11C]MET. Besides the short lived carbon-11 label, application of these radiotracers is also limited due to challenges related to data quantification. This is mainly due to the amino acids involvement in process other than protein synthesis for which reason the goal of this project was to develop a non-amino acid based PET radiotracer for imaging protein synthesis. As an inhibitor of protein synthesis puromycin was selected and small library of about 15 derivatives was prepared and evaluated in vitro to establish the most promising candidate. Detailed preclinical in vivo evaluation of the candidate [18F]FEPURO is currently being carried out in our laboratory.

 

Taken from: Betts et al, J. Med. Chem, 2016, 59(20), 9422
Taken from: Betts et al, J. Med. Chem, 2016, 59(20), 9422