Synthesis and biological evaluation of N-(2-[(18)F]Fluoropropionyl)-L-methionine for tumor imaging

Nuclear Medicine and Biology
Kong-Zhen HuXiaolan Tang

Abstract

N-position radiolabeled amino acids, such as N-(2-[(18)F]fluoropropionyl)-L-methionine ([(18)F]FPMET) as a derivative of L-methionine (MET), can potentially serve as a PET tracer for tumor imaging. In the current study, radiosynthesis and biological evaluation of [(18)F]FPMET as a new PET tumor agent are performed. [(18)F]FPMET was synthesized by reacting 4-nitrophenyl 2-[(18)F]fluoropropionate ([(18)F]NFP) with MET. In vitro competitive inhibition and protein incorporation experiments were performed with Hepa1-6 hepatoma cell lines. The biodistribution of [(18)F]FPMET was determined in S180 fibrosarcoma-bearing mice. PET/CT studies of [(18)F]FPMET were conducted in S180 fibrosarcoma-bearing mice, A549 lung adenocarcinoma-bearing nude mice, and PC-3 prostate cancer-bearing nude mice. [(18)F]FPMET was synthesized in 72%± 4% uncorrected radiochemical yield (n=10) from [(18)F]NFP. In vitro experiments showed that [(18)F]FPMET was primarily transported through Na(+)-dependent system A, system ASC, and system B(0,+), and was not incorporated into protein. Biodistribution and PET/CT imaging studies indicated that [(18)F]FPMET could delineate S180 fibrosarcoma, A549 lung adenocarcinoma, and PC-3 prostate cancer. An efficient synthesis...Continue Reading

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Citations

Jan 28, 2014·Apoptosis : an International Journal on Programmed Cell Death·Shaobo YaoLinquan Zang
Jun 14, 2017·Chemical Society Reviews·Dion van der BornDanielle J Vugts
Oct 25, 2016·Nuclear Medicine Communications·Shanzhen HeXiang Liang
Apr 1, 2020·Journal of Labelled Compounds & Radiopharmaceuticals·Fuhua WenGanghua Tang
Nov 17, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sheng-You LiWei-Dong Pan
Nov 20, 2020·Journal of Pharmaceutical Sciences·Anshul GuptaGaurav K Jain
Oct 4, 2016·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·David M SchusterStefano Fanti
Jun 27, 2015·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Kongzhen HuDahong Nie

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