Positron Emission Tomography Imaging of Drug-Induced Tumor Apoptosis with a Caspase-Triggered Nano-aggregation Probe

摘要

An 18F-labeled caspase-3 sensitive nano-aggregation PET tracer ([18F]CSNAT) was prepared and evaluated for imaging caspase-3 activity in doxorubicin-treated tumor xenografts. This enzyme-activatable PET tracer is designed to function in a novel mechanism – enhanced retention of the 18F activity in apoptotic tumors is achieved through intramolecular macrocyclization and in situ aggregation upon caspase-3 activation.