Nuclear　receptor　subfamily　4　group　A　member　1　(NR4A1;　also　termed　Nur77/TR3/NGFIB),　a　member　of　the　nuclear　receptor　superfamily,　is　expressed　as　an　early　response　gene　to　regulate　the　expression　of　multiple　target　genes.　Nur77　has　the　typical　structure　of　a　nuclear　receptor,　including　an　N-terminal　domain,　a　DNA　binding　domain,　and　a　ligand-binding　domain.　The　expression　and　localization　of　Nur77　are　closely　associated　with　its　roles　in　cell　proliferation　and　apoptosis.　Nur77　was　first　identified　as　an　orphan　receptor,　the　endogenous　ligand　of　which　has　not　yet　been　identified;　however,　an　increasing　number　of　compounds　targeting　Nur77　have　been　reported　to　have　beneficial　effects　in　the　treatment　of　cancer　and　other　diseases.　This　review　provides　a　brief　overview　of　the　identification,　structure,　expression　and　localization,　transcriptional　role　and　non-genomic　function　of　Nur77,　and　summarizes　the　ligands　that　have　been　shown　to　interact　with　Nur77,　including　cytosporone　B,　cisplatin,　TMPA,　PDNPA,　CCE9,　THPN,　Z-ligustilide,　celastrol　and　bisindole　methane　compounds,　which　may　potentially　be　used　to　treat　cancer　in　humans.