Targeting L-type amino acid transporter 1 for anticancer therapy: clinical impact from diagnostics to therapeutics

L-type amino acid transporter 1 (LAT1) is one of the amino acid transporters. It is overexpressed in various types of cancer cells, while it is produced restrictedly in normal tissues.We discuss its characteristics in cancer cells compared with normal cells. We also mention the current applications to target LAT1 for anticancer therapy focusing on prognostic biomarkers, radio-labeled tumor imaging reagents, amino acid-stapled prodrugs, LAT1-mediated enhanced transport of anticancer drugs and LAT1 inhibitors.LAT1 can be a versatile target to promisingly develop transporter-based drugs with enhanced drug delivery potential for anticancer therapy.