Radiotracer stereochemistry affects substrate affinity and kinetics for improved imaging of system x_C^- in tumors.

ABSTRACT: Amino acid utilization is perturbed in cancer cells, which rewire their metabolism to support cell survival and proliferation. This metabolic reprogramming can be exploited for diagnostic purposes through positron emission tomography imaging of fluorine-18 labeled amino acids. Despite its promise, little is known regarding transporter-recognition of non-natural amino acid stereoisomers or their utility for cancer imaging. We report here the synthesis and in vivo characterization of a radiolabeled amino acid (R)-4-(3-¹⁸F-fluoropropyl)-ʟ-glutamate ([¹⁸F]FRPG) and compared its tumor imaging properties to the 4S-isomer, [¹⁸F]FSPG. Methods: [¹⁸F]FRPG and [¹⁸F]FSPG uptake was assessed in H460 lung cancer ce

SUBMITTER: Greenwood HE 

PROVIDER: S-EPMC8825600 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature