The synthesis of pteroyl-lys conjugates and its application as Technetium-99m labeled radiotracer for folate receptor-positive tumor targeting |
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| Authors: | Guo Hongjuan Xie Fang Zhu Meilin Li Yan Yang Zhi Wang Xuebin Lu Jie |
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| Institution: | a Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China
b Key laboratory of Carcinogenesis and Translational Research (Ministry of Education), Breast Center, Peking University School of Oncology, Beijing Cancer Hospital and Institute, Beijing 100142, PR China |
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| Abstract: | Aiming to develop a new 99mTc-labeled folate derivative for FR-positive tumor imaging, a simpler method has been established to synthesize the folate-drug conjugates with free α-carboxyl group. In this study, the conjugate pteroyl-lys-HYNIC was synthesized and labeled with 99mTc using tricine and TPPTS as co-ligands. The radiochemical purity of the final complex 99mTc(HYNIC-lys-pteroyl)(tricine/TPPTS), 5 was high (>98%), and it remained stable in saline and plasma over 6 h after preparation. The biologic evaluation results showed that the 99mTc labeled pteroyl-lys conjugate was able to specifically target the FR-positive tumor cells and tissues both in vitro and in vivo, highlighting its potential as an effective folate receptor targeted agent for tumor imaging. |
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| Keywords: | 99mTc Folate receptor Folate-drug conjugates Pteroyl-lys-HYNIC Tumor imaging |
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