Abstract
Among amino acid transporters upregulated in tumor cells, LAT1 (SLC7A5) is the most favorable for the drug delivery to cancers due to its cancer-selective expression and broad substrate selectivity. LAT1 is responsible for the cancer delivery of anti-tumor phenylalanine-mustard melphalan and L-p-boronophenylalanine used for boron neutron capture therapy. LAT1 is also a target of PET imaging probe delivery. Most of amino acid probes target LAT1, whereas only FAMT is LAT1-selective. FAMT, therefore, exhibits the most remarkable cancer-selective accumulation. Cancer-selective drug design including the idea of amino acid-based pro-drugs would be possible based on the LAT1-selectivity and property as a LAT1 substrate.
