This review focuses on the amino acid transporters ASCT2, LAT1, xCT, SNAT1, SNAT2, and PAT1, which all have been implicated in cancer and spans well-explored (ASCT2, LAT1, xCT) and less explored (SNAT1, SNAT2, PAT1) SLCs in terms of structural biology and inhibitor identification. The gene discussed is SLC38A2; the disease is cancer.