2. Academic Validation
  3. Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor

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

  • ACS Med Chem Lett. 2016 Sep 28;7(12):1024-1027. doi: 10.1021/acsmedchemlett.6b00180.
Yang He 1,  Meng Wu 1,  Yangguang Liu 1,  Quanjie Li 1,  Xiaoyu Li 1,  Laixing Hu 1,  Shan Cen 1,  Jinming Zhou 1
Affiliations

Affiliation

  • 1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science , Beijing, China.
PMID: 27994731 DOI: 10.1021/acsmedchemlett.6b00180
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.

Keywords

Androgen receptor; gene report system; traditional Chinese medicine; triptophenolide.

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