Abstract
Background: Breast cancer is a malignant disease with high mortality rate among women in the world. It is necessary to diagnose breast cancer at the early stage before it metastasizes in patients.
Objective: The aim of this study is the evaluation of 99mTc-(tricine)-HYNIC-Lys-FROP for breast tumor imaging.
Method: Lys-FROP peptide was labeled with 99mTc using HYNIC as chelator and tricine as co-ligand. Specific binding of this radiolabeled peptide on breast cancerous cell was assessed in different cell lines as well as in tumor-bearing mice.
Results: HYNIC-Lys-FROP peptide was labeled with 99mTc at radiochemical purity more than 99%. It was observed high stability in normal saline and serum about 95%. The highest cellular uptake was observed in MCF-7 breast tumor cells treated with 99mTc-(tricine)-HYNIC-Lys-FROP as compared to other cell lines (lung, ovarian, T47D breast cancer cell lines). Biodistribution results in female MCF-7 tumor-bearing mice showed the relatively high tumor uptake and tumor-muscle ratio as 3.82 ± 0.66 after 15 min post-injection of 99mTc-(tricine)- HYNIC-Lys-FROP. Tumor uptake was reduced in mice that were co-injected with excess of unlabeled peptide to be 0.91 ± 0.08.
Conclusion: Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of breast cancer.
Keywords: Breast cancer, FROP peptide, radiopharmaceutical, tumor targeting, 99mTc, breast tumor.
Anti-Cancer Agents in Medicinal Chemistry
Title:99mTc-(tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting
Volume: 18 Issue: 9
Author(s): Sajjad Ahmadpour, Zohreh Noaparast, Seyed Mohammad Abedi and Seyed Jalal Hosseinimehr*
Affiliation:
- Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari,Iran
Keywords: Breast cancer, FROP peptide, radiopharmaceutical, tumor targeting, 99mTc, breast tumor.
Abstract: Background: Breast cancer is a malignant disease with high mortality rate among women in the world. It is necessary to diagnose breast cancer at the early stage before it metastasizes in patients.
Objective: The aim of this study is the evaluation of 99mTc-(tricine)-HYNIC-Lys-FROP for breast tumor imaging.
Method: Lys-FROP peptide was labeled with 99mTc using HYNIC as chelator and tricine as co-ligand. Specific binding of this radiolabeled peptide on breast cancerous cell was assessed in different cell lines as well as in tumor-bearing mice.
Results: HYNIC-Lys-FROP peptide was labeled with 99mTc at radiochemical purity more than 99%. It was observed high stability in normal saline and serum about 95%. The highest cellular uptake was observed in MCF-7 breast tumor cells treated with 99mTc-(tricine)-HYNIC-Lys-FROP as compared to other cell lines (lung, ovarian, T47D breast cancer cell lines). Biodistribution results in female MCF-7 tumor-bearing mice showed the relatively high tumor uptake and tumor-muscle ratio as 3.82 ± 0.66 after 15 min post-injection of 99mTc-(tricine)- HYNIC-Lys-FROP. Tumor uptake was reduced in mice that were co-injected with excess of unlabeled peptide to be 0.91 ± 0.08.
Conclusion: Findings showed this radiolabeled peptide is a promising candidate for tumor targeting and molecular imaging of breast cancer.
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Cite this article as:
Ahmadpour Sajjad , Noaparast Zohreh , Abedi Mohammad Seyed and Hosseinimehr Jalal Seyed *, 99mTc-(tricine)-HYNIC-Lys-FROP Peptide for Breast Tumor Targeting, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (9) . https://dx.doi.org/10.2174/1871520618666180307142027
DOI https://dx.doi.org/10.2174/1871520618666180307142027 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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