Synthesis and Evaluation of 99mTc-Labeled Dimeric Folic Acid for FR-Targeting
AbstractThe folate receptor (FR) is overexpressed in a wide variety of human tumors. In our study, the multimeric concept was used to synthesize a dimeric folate derivative via a click reaction. The novel folate derivative (HYNIC-D1-FA2) was radiolabeled with 99mTc using tricine and trisodium triphenylphosphine-3,3′,3″-trisulfonate (TPPTS) as coligands (99mTc-HYNIC-D1-FA2) and its in vitro physicochemical properties, ex vivo biodistribution and in vivo micro-SPECT/CT imaging as a potential FR targeted agent were evaluated. It is a hydrophilic compound (log P = −2.52 ± 0.13) with high binding affinity (IC50 = 19.06 nM). Biodistribution in KB tumor-bearing mice showed that 99mTc-HYNIC-D1-FA2 had high uptake in FR overexpressed tumor and kidney at all time-points, and both of them could obviously be inhibited when blocking with free FA in the blocking studies. From the in vivo micro-SPECT/CT imaging results, good tumor uptake of 99mTc-HYNIC-D1-FA2 was observed in KB tumor-bearing mice and it could be blocked obviously. Based on the results, this new radiolabeled dimeric FA tracer might be a promising candidate for FR-targeting imaging with high affinity and selectivity. View Full-Text
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Guo, Z.; Gao, M.; Song, M.; Shi, C.; Zhang, P.; Xu, D.; You, L.; Zhuang, R.; Su, X.; Liu, T.; Du, J.; Zhang, X. Synthesis and Evaluation of 99mTc-Labeled Dimeric Folic Acid for FR-Targeting. Molecules 2016, 21, 817.
Guo Z, Gao M, Song M, Shi C, Zhang P, Xu D, You L, Zhuang R, Su X, Liu T, Du J, Zhang X. Synthesis and Evaluation of 99mTc-Labeled Dimeric Folic Acid for FR-Targeting. Molecules. 2016; 21(6):817.Chicago/Turabian Style
Guo, Zhide; Gao, Mengna; Song, Manli; Shi, Changrong; Zhang, Pu; Xu, Duo; You, Linyi; Zhuang, Rongqiang; Su, Xinhui; Liu, Ting; Du, Jin; Zhang, Xianzhong. 2016. "Synthesis and Evaluation of 99mTc-Labeled Dimeric Folic Acid for FR-Targeting." Molecules 21, no. 6: 817.
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