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.
Highlights
Positron emission tomography (PET) provides noninvasive images of physiologic function and is regularly used in the diagnosis and staging of cancer [1]
We examine the biological evaluation of [18F]FPGLU For single-isotope (18F)]FPGLU as a stable PET tracer for tumor imaging
No-carrier-added 18F-fluoride was obtained through the nuclear reaction 18O(p, n)18F by irradiation of more than 95% [18O]enriched water target with 10-MeV proton beam on the Cyclone 10/5 cyclotron (IBA Technologies, Belgium)
Summary
Positron emission tomography (PET) provides noninvasive images of physiologic function and is regularly used in the diagnosis and staging of cancer [1]. [18F]FDG has a high uptake into the brain and nonmalignant, inflammatory cellular elements [3]. To be able to overcome these disadvantages, work has been conducted to identify new tracers for tumor imaging that has greater sensitivity and better specificity for tumor imaging. Since tumor growth and proliferation require a high amount of energy and specific amino acids, positron-emitting radionuclide-labeled amino acids can be potential alternatives for tumor imaging. S-[11C]methyl-L-methionine ([11C]MET) and O-2-[18F]fluoroethyl-L-tyrosine ([18F]FET) are commonly used amino acid tracer for the in vivo targeting of brain tumors [7]. One of the major limitations of extracranial tumor imaging with [11C]MET or [18F]FET has relative poor tumor uptake, producing low to moderate tumor to background ratios [8]
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