Synthesis and evaluation of an in vivo imaging probe for tumor based on the intracellular transporting system

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Peptide transporter-1(PEPT1) is expected to be a target for the tumor-selective molecular delivery. Because several phenylalanine-containing dipeptides are well recognized by PEPT1 as substrates, we designed and synthesized a peptidergic compound consisting of 2-[^<18> F] fluoronicotinic acid and phenylalanine(2-[^<18> F] FNA-Phe) as a PET probe for tumor imaging. The uptake to human pancreatic tumor cells(AsPC-1) that expresses PEPT1 was measured in vitro, which demonstrated that 2-[^<18> F] FNA-Phe was taken up into cells via PEPT1. When 2-[^<18> F] FNA-Phe was intravenously injected to BALB/c nude mice bearing AsPC-1, the tumor was clearly visualized.