Amino acids (AAs) are important nutrients for proliferating tumor cells, and amino acid
transport is generally increased in many malignant tumor cells. So far, as a complementary category to
18F-2-fluoro-2-deoxy-D-glucose ([18F]FDG), radiolabeled amino acids that target the upregulated level
of amino acid transport have been successfully employed for tumor imaging for decades, thanks to
their better differentiation between tumor lesions and inflammation. This review summarizes the development
of various radiolabeled amino acid analogues for tumor imaging with single photon emission
computed tomography (SPECT) and positron emission tomography (PET) and introduces the basic
data related to this area, such as the biological basis, chemical structure, radiolabeling, preclinical
evaluation and clinical application. In addition, current status and future prospects of this class of imaging
agents are discussed in this review.
Keywords: Amino acids, PET, radiopharmaceuticals, SPECT, tumor imaging, tumor.
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