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Radiolabeled apoptosis imaging agents for early detection of response to therapy
1Division of Pharmaceutical Sciences, Graduate School of Medical Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
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.
Insights
Molecular imaging of apoptosis detects therapeutic effects early. This review covers traditional protein-based agents and newer, low-molecular-weight apoptosis imaging agents with improved properties.
Area of Science:
- Molecular imaging
- Oncology
- Apoptosis research
Background:
- Apoptosis (programmed cell death) is crucial for homeostasis and therapy response.
- Molecular imaging of apoptotic cells aids in early detection of therapeutic effects, especially in cancer.
- Radiolabeled annexin V compounds have been the standard for in vivo apoptosis imaging.
Purpose of the Study:
- To review the evolution of apoptosis imaging agents.
- To highlight the limitations of current protein-based agents.
- To explore promising low-molecular-weight alternatives for apoptosis imaging.
Main Methods:
- Comprehensive literature review of apoptosis imaging agents.
- Analysis of radiolabeled annexin V compounds and their drawbacks.
- Examination of novel low-molecular-weight apoptosis imaging agents.
Main Results:
- Protein-based agents like annexin V have disadvantages such as slow clearance and immunogenicity.
- Several low-molecular-weight apoptosis imaging agents have been developed.
- Promising agents include radiolabeled peptides, bis(zinc(II)-dipicolylamine) complexes, ML-10, caspase-3 activity agents, duramycin, and phosphonium cations.
Conclusions:
- Low-molecular-weight agents offer potential advantages over traditional protein-based apoptosis imaging agents.
- These novel agents could improve the early detection of therapeutic responses in oncology.
- Further research into these agents is warranted for clinical application.
