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Repurposing an atherosclerosis targeting peptide for tumor imaging
Luciana Kovacs1, Ryan A Davis2, Tanushree Ganguly2
1Department of Internal Medicine, Division of Hematology/Oncology, University of California Davis, 2921 Stockton Blvd, Sacramento, CA 95817, USA.
Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|December 5, 2021
Summary
A novel peptide (CTHRSSVVC) previously targeting atherosclerosis showed accumulation in 4T1 tumors in mice. While not binding macrophages in vitro, this peptide demonstrates potential as a tumor imaging agent.
Area of Science:
- Oncology
- Cardiovascular Research
- Biomedical Imaging
Background:
- Cancer and atherosclerosis share pathological features like uncontrolled cell proliferation and inflammation.
- A peptide (CTHRSSVVC) known to bind atherosclerotic lesions was investigated for tumor-homing capabilities.
Purpose of the Study:
- To evaluate the tumor-targeting potential of the CTHRSSVVC peptide in a preclinical cancer model.
- To assess if a peptide targeting atherosclerosis could be repurposed for cancer imaging.
Main Methods:
- Synthesis of N-terminally sulfo-Cy5 labeled CTHRSSVVC peptide.
- In vitro evaluation of macrophage binding using flow cytometry and immunofluorescence.
- In vivo tumor targeting assessment in 4T1 tumor-bearing mice using optical imaging and ex vivo confocal microscopy.
Main Results:
- The sulfo-Cy5-CTHRSSVVC peptide showed no selective binding to macrophages in vitro.
- In vivo, the peptide accumulated in 4T1 tumors, achieving a tumor-to-normal tissue ratio of 7.21 ± 1.44 at 2 hours post-injection.
- Ex vivo analysis indicated peptide accumulation in the tumor stroma, specifically in regions with spindle-shaped cells.
Conclusions:
- The CTHRSSVVC peptide demonstrates in vivo tumor accumulation, suggesting potential for tumor imaging.
- Further research is needed to identify the specific molecular target of the CTHRSSVVC peptide within the tumor microenvironment.

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