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Looking for a PET Tracer for Imaging Apoptosis
* 1 , 1 , 2 , 2 , 1 , 1
1  PET/Biomedical Cyclotron Unit and Department of Nuclear Medicine, Erasme Hoapital, Université Libre de Bruxelles, Belgium
2  Laboratory of Immunobiology Institute for Molecular Biology and Medicine Université Libre de Bruxelles (IBMM, ULB)

Published: 02 November 2015 by MDPI in 1st International Electronic Conference on Medicinal Chemistry session ECMC-1

In multicellular organisms, homeostasis is maintained by a balance between cell proliferation and apoptosis (programmed cell death). It is a physiological form of cell death responsible for the deletion of non-repairable damaged, mutated, or cells which have lost their function.

We describe the synthesis of a series of potential inhibitors of caspases from a modified aspartic acid residue (fluoromethylketone, fmk). The addition to the entire series of, 3-cyano-4-fluoro-benzoyl- pattern on one hand or of, 4-fluoro-2-thiazolamino- pattern on the other hand will subsequently allow the introduction of a PET isotope (18F).

In order to determine potential candidates, the inhibitory activity of these compounds was evaluated in vitro on a series of human T cells compared to the z-VAD-fmk as a reference.

Keywords: Apoptosis; cell death; radiochemistry; PET