The　solute　carrier　(SLC)　family,　with　more　than　400　membrane　-bound　proteins,　facilitates　the　transport　of　a　wide　array　of　substrates　such　as　nutrients,　ions,　metabolites,　and　drugs　across　biological　membranes.　Amino　acid　transporters　(AATs)　are　membrane　transport　proteins　that　mediate　transfer　of　amino　acids　into　and　out　of　cells　or　cellular　organelles.　AATs　participate　in　many　important　physiological　functions　including　nutrient　supply,　metabolic　transformation,　energy　homeostasis,　redox　regulation,　and　neurological　regulation.　Several　AATs　have　been　found　to　significantly　impact　the　progression　of　human　malignancies,　and　dysregulation　of　AATs　results　in　metabolic　reprogramming　affecting　tumor　growth　and　progression.　However,　current　clinical　therapies　that　directly　target　AATs　have　not　been　developed.　The　purpose　of　this　review　is　to　highlight　the　structural　and　functional　diversity　of　AATs,　the　molecular　mechanisms　in　human　diseases　such　as　tumors,　kidney　diseases,　and　emerging　therapeutic　strategies　for　targeting　AATs.