ArticleNuclear medicine and biology2015
System a amino acid transport-targeted brain and systemic tumor PET imaging agents 2-amino-3-[(18)F]fluoro-2-methylpropanoic acid and 3-[(18)F]fluoro-2-methyl-2-(methylamino)propanoic acid.
Article in Nuclear medicine and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Preclinical Comparison ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2026Article
- PET Imaging of System A Amino Acid Transport Detects Early Response to Immune Checkpoint Inhibitor Therapy in a Syngeneic Mouse Model.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2025Article
- The Role of Amino Acids in the Diagnosis, Risk Assessment, and Treatment of Breast Cancer: A Review.Current issues in molecular biology · 2023Review
- Preclinical and Clinical Use of Indigenously DevelopedACS pharmacology & translational science · 2023Review
- The Utility of Conventional Amino Acid PET Radiotracers in the Evaluation of Glioma Recurrence also in Comparison with MRI.Diagnostics (Basel, Switzerland) · 2022Review
- Synthesis, Radiolabeling, and Biological Evaluation of theACS pharmacology & translational science · 2021Article
- Amino Acid Metabolism as a Target for Breast Cancer Imaging.PET clinics · 2018Review
- Amino acid transport system - A substrate predicts the therapeutic effects of particle radiotherapy.PloS one · 2017Article
- PET Tracers Beyond FDG in Prostate Cancer.Seminars in nuclear medicine · 2016Review
- Article
- Synthesis and Biological Evaluation of (S)-Amino-2-methyl-4-[(76)Br]bromo-3-(E)-butenoic Acid (BrVAIB) for Brain Tumor Imaging.Journal of medicinal chemistry · 2015Article
- Synthesis, Radiolabeling, and Biological Evaluation of (R)- and (S)-2-Amino-5-[(18)F]fluoro-2-methylpentanoic Acid ((R)-, (S)-[(18)F]FAMPe) as Potential Positron Emission Tomography Tracers for Brain Tumors.Journal of medicinal chemistry · 2015Article
- Imaging tumor metabolism using positron emission tomography.Cancer journal (Sudbury, Mass.)Review
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4 authors.
Funding
Abstract
introductionAmino acid based radiotracers target tumor cells through increased uptake by membrane-associated amino acid transport (AAT) systems. In the present study, four structurally related non-natural (18)F-labeled amino acids, (R)- and (S)-[(18)F]FAMP 1 and (R)- and (S)-[(18)F]MeFAMP 2 have been prepared and evaluated in vitro and in vivo for their potential utility in brain and systemic tumor imaging based upon primarily system A transport with positron emission tomography (PET).
methodsThe transport of enantiomers of [(18)F]FAMP 1 and [(18)F]MeFAMP 2 was measured through in vitro uptake assays in human derived cancer cells including A549 (lung), DU145 (prostate), SKOV3 (ovary), MDA MB468 (breast) and U87 (brain) in the presence and absence of amino acid transporter inhibitors. The in vivo biodistribution of these tracers was evaluated using tumor mice xenografts at 15, 30, 60 and 120 min post injection.
resultsAll four tracers showed moderate to high levels of uptake (1-9%ID/5×10(5) cells) by the cancer cell lines tested in vitro. AAT cell inhibition assays demonstrated that (R)-[(18)F]1 and (S)-[(18)F]1 entered these tumor cells via mixed AATs, likely but not limited to system A and system L. In contrast, (R)-[(18)F]2 and (S)-[(18)F]2 showed high selectivity for system A AAT. Similar to the results of in vitro cell studies, the tumor uptake of all four tracers was good to high and persisted over the 2 hours time course of in vivo studies. The accumulation of these tracers was higher in tumor than most normal tissues including blood, brain, muscle, bone, heart, and lung, and the tracers with the highest in vitro selectivity for system A AAT generally demonstrated the best tumor imaging properties. Higher uptake of these tracers was observed in the pancreas, kidney and spleen compared to tumors.
conclusionsThese preclinical studies demonstrate good imaging properties in a wide range of tumors for all four amino acids evaluated with (R)-[(18)F]2 having the highest selectivity for system A AAT.
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