Preclinical evaluation of an ¹⁸F-labeled N^ε-acryloyllysine piperazide for covalent targeting of transglutaminase 2.

ABSTRACT:

Background

Transglutaminase 2 (TGase 2) is a multifunctional protein and has a prominent role in various (patho)physiological processes. In particular, its transamidase activity, which is rather latent under physiological conditions, gains importance in malignant cells. Thus, there is a great need of theranostic probes for targeting tumor-associated TGase 2, and targeted covalent inhibitors appear to be particularly attractive as vector molecules. Such an inhibitor, equipped with a radionuclide suitable for noninvasive imaging, would be supportive for answering the general question on the possibility for functional characterization of tumor-associated TGase 2. For this purpose, the recently developed ¹⁸F-labeled N^ε-acryloyllysine piperazide [¹⁸F]7b,

SUBMITTER: Wodtke R 

PROVIDER: S-EPMC10761660 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature