Abstract
Since apoptosis plays an important role in maintaining homeostasis and is associated with responses to therapy, molecular imaging of apoptotic cells could be useful for early detection of therapeutic effects, particularly in oncology. Radiolabeled annexin V compounds are the hallmark in apoptosis imaging in vivo. These compounds are reviewed from the genesis of apoptosis (cell death) imaging agents up to recent years. They have some disadvantages, including slow clearance and immunogenicity, because they are protein-based imaging agents. For this reason, several studies have been conducted in recent years to develop low molecule apoptosis imaging agents. In this review, radiolabeled phosphatidylserine targeted peptides, radiolabeled bis(zinc(II)-dipicolylamine) complex, radiolabeled 5-fluoropentyl-2-methyl-malonic acid (ML-10), caspase-3 activity imaging agents, radiolabeled duramycin, and radiolabeled phosphonium cation are reviewed as promising low-molecular-weight apoptosis imaging agents.
Highlights
Apoptosis is known to play an important role in maintaining homeostasis; it is associated with several diseases and responses to therapy
Blankenberg et al reported the use of 99mTc-labeled annexin V, which has hydrazinonicotinamide (HYNIC) as a ligand for technetium, for apoptosis imaging [8]
Many studies have demonstrated that 99mTcHYNIC-annexin V accumulates in apoptotic cells and can be used to visualize apoptosis in animal models [12,13,14,15]. 99mTcHYNIC-annexin V can be considered as a benchmark in the field of apoptosis imaging, as the easy labeling method has made this tracer the most extensively investigated and the best characterized apoptosis-detecting radioligand [16]
Summary
Apoptosis is known to play an important role in maintaining homeostasis; it is associated with several diseases and responses to therapy. Molecular imaging of apoptotic cells could be useful for elucidation of the diseases and early detection of therapeutic effects and could contribute to personalized medicine. We introduce radiolabeled compounds for molecular imaging of apoptosis (cell death), their applications, and utility in medicine
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