雄激素受体在前列腺癌的发生和发展中作用明确。临床上用于治疗前列腺癌的药物为雄激素受体配体结合域的竞争性抑制剂。然而，这类药物的疗效因患者表现出现抵抗而受到限制，导致疾病发展为去势抵抗性前列腺癌。近年来靶向雄激素受体N-端结合域或DNA结合域的药物被报道，这些药物能够克服当前药物治疗的缺点，目前正在临床研究中。对不同靶向的非甾体类雄激素受体的研究进展进行综述。

The role of androgen receptor in the initiation and progression of prostate cancer is well established. Competitive inhibition of the androgen receptor ligand-binding domain has been employed to combat the disease in clinic. However, their efficacy has often been limited by the emergence of resistance, as a result, leading to disease development for castration-resistant prostate cancer. In recent years, targeting drugs of amino-terminal domain or DNA-binding domain of the androgen receptor have been reported, which can overcome the shortcomings of current drugs, and the clinical research on these drugs is now underway. Research progress on targeted drugs of non-steroidal androgen receptor is reviewed in this paper.

中国医学科学院医学与健康科技创新工程项目（2016-I2M-3-022、2017-I2M-3-019）