Development of caspase-3-selective activity-based probes for PET imaging of apoptosis.

ABSTRACT:

Background

The cysteine-aspartic acid protease caspase-3 is recognized as the main executioner of apoptosis in cells responding to specific extrinsic and intrinsic stimuli. Caspase-3 represents an interesting biomarker to evaluate treatment response, as many cancer therapies exert their effect by inducing tumour cell death. Previously developed caspase-3 PET tracers were unable to reach routine clinical use due to low tumour uptake or lack of target selectivity, which are two important requirements for effective treatment response evaluation in cancer patients. Therefore, the goal of this study was to develop and preclinically evaluate novel caspase-3-selective activity-based probes (ABPs) for apoptosis imaging.

Results

A library of caspase-3-selective ABPs was developed for

SUBMITTER: Lauwerys L 

PROVIDER: S-EPMC11310375 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature