Selective L-type amino acid transporter 1 inhibitor (LAT1 or SLC7A5, IC50 = 140 nM for 14C-leucine uptake in S2-hLAT1 cells, and 60 nM for HT29 human colon adenocarcinoma cells: growth inhibition IC50s = 16.4 µM and 4.1 µM respectively for S2 and HT29 cells).1 Also active in HT-29 mouse xenograft models. JPH203 is active in a variety of cancer models and has progressed to clinical trials.2 It sensitized A549 and MIA Paca-2 cells to radiation by enhancing cellular senescence via mTOR downregulation3 and sensitized EGFR-expressing cancer cell lines to gefitinib therapy4. JPH203 treatment of non-small cell lung cancer cells led to downregulation of PD-L1 suggesting that LAT1 inhibition may help overcome the immune suppressive tumor microenvironment.5
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