Synthesis and biological evaluation of 68Ga‐labeled Pteroyl‐Lys conjugates for folate receptor‐targeted tumor imaging |
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| Authors: | Yingfang He Chun Zhang Hua Zhu Zhi Yang Jie Lu |
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| Affiliation: | 1. Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, PR China;2. Department of Nuclear Medicine, Beijing Chao‐Yang Hospital, Capital Medical University, Beijing, PR China;3. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital and Institute, Beijing, PR China |
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| Abstract: | ![]()
In order to develop novel 68Ga‐labeled PET tracers for folate receptor imaging, two DOTA‐conjugated Pteroyl‐Lys derivatives, Pteroyl‐Lys‐DOTA and Pteroyl‐Lys‐DAV‐DOTA, were designed, synthesized and radiolabeled with 68Ga. Biological evaluations of the two radiotracers were performed with FR‐positive KB cell line and athymic nude mice bearing KB tumors. Both 68Ga‐DOTA‐Lys‐Pteroyl and 68Ga‐DOTA‐DAV‐Lys‐Pteroyl exhibited receptor specific binding in KB cells in vitro. The tumor uptake values of 68Ga‐DOTA‐Lys‐Pteroyl and 68Ga‐DOTA‐DAV‐Lys‐Pteroy were 10.06 ± 0.59%ID/g and 11.05 ± 0.60%ID/g at 2 h post‐injection, respectively. Flank KB tumor was clearly visualized with 68Ga‐DOTA‐DAV‐Lys‐Pteroyl by Micro‐PET imaging at 2 h post‐injection, suggesting the feasibility of using 68Ga‐labeled Pteroyl‐Lys conjugates as a novel class of FR targeted probes. |
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| Keywords: | radiopharmaceutical 68Ga folate receptor Pteroyl‐Lys PET |
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