Abstract: Prostate cancer is a malignant tumor with an extremely high rate of incidence and mortality in male.The occurrence and development of prostate cancer are closely related to androgen receptor (AR)-mediated signaling pathway.AR gene amplification, mutation and splice variant expression have posed the problem of drug resistance for the treatment of prostate cancer.Therefore, it is urgent to discover novel targets to overcome clinical drug resistance of prostate cancer.Studies have shown that, besides AR, other members of the nuclear receptors are also closely related to the occurrence and progression of prostate cancer.Small molecule drugs targeting these nuclear receptors against prostate cancer have been studied in preclinical or clinical research.This paper reviews the mechanisms of action of these nuclear receptors in prostate cancer and the research progress of related small molecule compounds.