Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor

详细信息    查看全文

• 作者：Yang He ; Meng Wu ; Yangguang Liu ; Quanjie Li ; Xiaoyu Li ; Laixing Hu ; Shan Cen ; Jinming Zhou
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：December 8, 2016
• 年：2016
• 卷：7
• 期：12
• 页码：1024-1027
• 全文大小：312K
• ISSN：1948-5875

文摘

A compound, triptophenolide, derived from Tripterygium wilfordii was identified as an antiandrogen. Triptophenolide inhibits the activity of both wild-type and F876L mutant androgen receptors. Triptophenolide exhibits its antiandrogenic activity through competitive binding with androgen in the hormone-binding pocket, decreasing the expression of androgen receptor, and reducing the nuclear translocation of androgen receptor.