title: Radiosynthesis and biological evaluation of N-[18F]labeled glutamic acid as a tumor metabolic imaging tracer.
abstract: We have previously reported that N-(2-[18F]fluoropropionyl)-L-methionine ([18F]FPMET) selectively accumulates in tumors. However, due to the poor pharmacokinetics of [18F]FPMET in vivo, the potential clinical translation of this observation is hampered. In this study, we rationally designed and synthesized [18F] or [11C]labeled N-position L-glutamic acid analogues for tumor imaging. N-(2-[18F]fluoropropionyl)-L-glutamic acid ([18F]FPGLU) was synthesized with a 30±10% (n = 10, decay-corrected) overall radiochemical yield and a specific activity of 40±25 GBq/μmol (n = 10) after 130 min of radiosynthesis. In vitro cell experiments showed that [18F]FPGLU was primarily transported through the XAG(-) system and was not incorporated into protein. [18F]FPGLU was stable in urine, tumor tissues, and blood. We were able to use [18F]FPGLU in PET imaging and obtained high tumor to background ratios when visualizing tumors tissues in animal models.
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Kongzhen
authors.initials: K
authors.lastname: Hu
authors.affiliation: School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China.
authors.forename: Kan
authors.initials: K
authors.lastname: Du
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Ganghua
authors.initials: G
authors.lastname: Tang
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Shaobo
authors.initials: S
authors.lastname: Yao
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Hongliang
authors.initials: H
authors.lastname: Wang
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Liang
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Baoguo
authors.initials: B
authors.lastname: Yao
authors.affiliation: PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Huang
authors.affiliation: School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China.
authors.forename: Linquan
authors.initials: L
authors.lastname: Zang
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D003952:Diagnostic Imaging / Q000379:methods; D018698:Glutamic Acid / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D008715:Methionine / Q000737:chemistry; D051379:Mice; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000737:chemistry*; D014018:Tissue Distribution / Q000502:physiology
chemical_list: D019275:Radiopharmaceuticals; D018698:Glutamic Acid; D008715:Methionine