Evaluation of (2S,4S)-4-[¹⁸F]FEBGln as a Positron Emission Tomography Tracer for Tumor Imaging

Design, Synthesis, and Biological Evaluation of a Novel [18F]-Labeled Arginine Derivative for Tumor Imaging

“…This process is regulated by the type and expression level of amino acid transporters [16,17]. Therefore, based on this difference in amino acid demand, a series of radiopharmaceuticals have been developed [16,[18][19][20][21][22][23]. Arginine is an important substrate of cationic amino acid transport carriers and an important source of energy for a variety of tumors [24,25].…”

“…Micro PET imaging studies have shown that the tumor-tomuscle ratio of [ 18 F]FPARG is approximately 2 at 30, 60, 90, and 120 min in NCI-H1299 tumor-bearing mice. Our group designed, synthesized, and obtained the tracer (2S,4S)4-[ 18 F]FPArg by introducing a fluoropropyl group on carbon-4 of arginine [32]. The major difference between (2S,4S)4-[ 18 F]FPArg and the previous two tracers is that the modified site was carbon-4 of arginine, so the characteristic groups of arginine (amino, carboxyl, and guanidine) were retained.…”

“…Our group designed, synthesized, and obtained the tracer (2S,4S)4-[ 18 F]FPArg by introducing a fluoropropyl group on carbon-4 of arginine [32]. The major difference between (2S,4S)4-[ 18 F]FPArg and the previous two tracers is that the modified site was carbon-4 of arginine, so the characteristic groups of arginine (amino, carboxyl, and guanidine) were retained. Furthermore, the size of the modified group was smaller.…”

“…Furthermore, the size of the modified group was smaller. Based on these reasons, (2S,4S)4-[ 18 F]FPArg preserved the biological activity of arginine to the greatest extent. Breast cancer and glioma can be visualized with a high contrast through (2S,4S)4-[ 18 F]FPArg [32,33].…”

Design of Novel 18F-Labeled Amino Acid Tracers Using Sulfur 18F-Fluoride Exchange Click Chemistry

“…Therefore, the development of radiolabeled amino acids that target different types of amino acid transporters can provide more detailed and reliable information for the precise diagnosis and treatment of tumors. A series of 11 C- and 18 F-labeled tracers have been reported, including L-type tracers, [ 11 C]­MET, , ( S )-[ 18 F]­FET, − [ 18 F]­FDOPA, , [ 18 F]­FMT, and (2 S ,4 S )­4-[ 18 F]­FEBGln; ASC-type tracers, 5-[ 11 C]­Gln, (2 S ,4 R )­4-[ 18 F]­FGln, , anti -3-[ 18 F]­FACBC, and (2 S ,4 S )­4-[ 18 F]­FPGln; A-type tracers, [ 18 F]- cis -FPro, ( S )-[ 18 F]­FAMP, and ( S )-[ 18 F]­MeFAMP; X C – -type tracers, (2 S ,4 R )-4-[ 18 F]­FGlu, and (2 S ,4 S )­[ 18 F]­FSPG; and CAT-type tracers, (2 S ,4 S )­4-[ 18 F]­FPArg and ( S )-[ 18 F]­AFETP (Figure ). After decades of development, research on radiolabeled amino acids has made important progress, and [ 11 C]­MET, ( S )-[ 18 F]­FET, and [ 18 F]­FDOPA have been applied to the diagnosis of clinical brain tumors.…”