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

Yang He, Meng Wu, Yangguang Liu, Quanjie Li, Xiaoyu Li, Laixing Hu, Shan Cen, Jinming Zhou

ACS Med Chem Lett. 2016 Sep 28;7(12):1024-1027.

PMID: 27994731

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP74285862 Triptophenolide Triptophenolide 74285-86-2 Price
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