针对不同靶点的前列腺癌药物的研究进展  

Recent progress in new drugs aiming at different targets for prostate cancer

作　　者：陆旭芳[1] 敦康 孙迎迎[1] 李志裕[1] 

机构地区：[1]中国药科大学药学院,南京210009

出　　处：《中国新药杂志》2014年第11期1273-1278,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金(21372260)

摘　　要：睾酮和二氢睾酮能够与雄激素受体结合从而引发基因的转录和细胞的增殖,而雄激素产生过多容易引起前列腺癌的产生。目前很多研究旨在发现针对睾酮和二氢睾酮的生物合成过程中的酶以及雄激素受体上的结合位点来设计与合成具有活性的前列腺癌药物,然而目前很多药物的使用会容易引起去势抵抗性前列腺癌的发生。因此,寻找能治疗前列腺癌以至去势抵抗性前列腺癌的药物成为现在研究的热点,本文综述了雄激素的生物代谢以及雄激素受体的作用机制,以及针对不同靶点的药物研究进展。Androgen receptor promotes gene transcription in prostate cell growth and carcinogenesis of prostate cancer. And testosterone and dihydrotestosterone can act with androgen receptor to induce transcription. Recent studies indicated that targeting the enzymes in the biosynthesis of testosterone and dihydrotestosterone and even the binding site in androgen receptor may have clinical benefits. However, castration-resistant prostate cancer occurs after a long period use of prostate cancer drugs such as bicalutamide and nilutamide. Therefore, progress still needs to be made in order to find compounds with an improved efficiency in treating prostate cancer and castration-resistant prostate cancer. This review focuses on the androgen metabolism in the prostate and the action mechanism of androgen receptor to clarify the development of compounds for the treatment of prostate cancer.

关 键 词：雄激素受体 酶 代谢 进展 前列腺癌 靶点 

分 类 号：R979.1[医药卫生—药品]