Development of a novel 99mTc‐labeled small molecular antagonist for CXCR4 positive tumor imaging |
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| Authors: | Xuran Zhang Linyi You Shuting Chen Mengna Gao Zhide Guo Jin Du Jie Lu Xianzhong Zhang |
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| Affiliation: | 1. Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education;2. College of Chemistry, Beijing Normal University, Beijing, PR China;3. Department of Isotope, China Institute of Atomic Energy, Beijing, China;4. Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, Fujian, PR China |
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| Abstract: | The chemokine receptor 4 (CXCR4) has been an attractive molecular target for tumor imaging, because it is overexpressed in many tumor types and involved in tumor progression and metastasis. The purpose of this study is to examine the CXCR4 targeting properties of 99mTc‐labeled AMD3465, a small molecule antagonist of CXCR4. 99mTc‐AMD3465 was prepared in high yield (>95%) and stable in mice serum at least for 4 hours. In vitro cell binding experiments were performed with Chinese hamster ovary (CHO), MCF‐7 (breast cancer), and CHO‐CXCR4 (CHO stably transfected to express CXCR4) cell lines. Small animal single photon emission computed tomography/computed tomography imaging studies in nude mice bearing MCF‐7 and CHO xenografts showed that the uptakes of the radiotracer in MCF‐7 tumors were significantly higher than those in the CXCR4‐negative CHO tumors (P < 0.05), and the MCF‐7 tumors uptake could be blocked with an excess of unlabeled AMD3465 (P < 0.05). These results suggested that 99mTc‐AMD3465 could be a potential single photon emission computed tomography radiotracer for CXCR4 imaging. |
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| Keywords: | AMD3465 CXCR4 SPECT Technetium‐99m tumor imaging |
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