Alanine-serine-cysteine transporter 2 (ASCT2) is a glutamine (Gln) transporter that is required for cell proliferation and is overexpressed in tumors such as non-small-cell lung cancer (NSCLC). Researchers from China Pharmaceutical University have reported on the discovery and preclinical characterization of a novel series of ASCT2 inhibitors that led to the identification two lead compounds.