The transamidase
activity of transglutaminase 2 (TGase 2) is considered
to be important for several pathophysiological processes including
fibrotic and neoplastic tissue growth, whereas in healthy cells this
enzymatic function is predominantly latent. Methods that enable the
highly sensitive detection of TGase 2, such as application of radiolabeled
activity-based probes, will support the exploration of the enzyme’s
function in various diseases. In this context, the radiosynthesis
and detailed in vitro radiopharmacological evaluation
of an 18F-labeled N
ε-acryloyllysine
piperazide are reported. Robust and facile detection of the radiotracer-TGase
2 complex by autoradiography of thin layer plates and polyacrylamide
gels after chromatographic and electrophoretic separation owing to
irreversible covalent bond formation was demonstrated for the isolated
protein, cell lysates, and living cells. By use of this radiotracer,
quantitative data on the expression profile of activatable TGase 2
in mouse organs and selected tumors were obtained for the first time
by autoradiography of tissue sections.