Abstract: Radiotherapy has become one of the main approaches in cancer treatment. However, tumor have radioresistance and normal tissues have radiation tolerant doses, both seriously affect the effect of cancer radiotherapy. It is of importance to develop radiation sensitizers to improve the radiosensitivity of tumor cells. Nuclear receptors are a kind of transcription factor superfamily, which are abundantly expressed in cells and participates in various pathophysiological processes. Recent studies have suggested that nuclear receptors and their related ligands may play important roles in tumor radioresistanace, which provide novel targets for radiosensitization. In this review, the research progress of nuclear receptors and related ligands in tumor radiosensitization is discussed.