Literature DB >> 27994731

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

Yang He1, Meng Wu1, Yangguang Liu1, Quanjie Li1, Xiaoyu Li1, Laixing Hu1, Shan Cen1, Jinming Zhou1.   

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.

Entities:  

Keywords:  Androgen receptor; gene report system; traditional Chinese medicine; triptophenolide

Year:  2016        PMID： 27994731      PMCID： PMC5150686          DOI： 10.1021/acsmedchemlett.6b00180

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  20 in total

Review 1.  Triptolide in the treatment of psoriasis and other immune-mediated inflammatory diseases.

Authors:  Rui Han; Martin Rostami-Yazdi; Sascha Gerdes; Ulrich Mrowietz
Journal:  Br J Clin Pharmacol       Date:  2012-09       Impact factor: 4.335

Review 2.  Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis.

Authors:  Howard I Scher; Charles L Sawyers
Journal:  J Clin Oncol       Date:  2005-11-10       Impact factor: 44.544

Review 3.  A Chinese herb Tripterygium wilfordii Hook F in the treatment of rheumatoid arthritis: mechanism, efficacy, and safety.

Authors:  Jun Bao; Sheng-Ming Dai
Journal:  Rheumatol Int       Date:  2011-03-02       Impact factor: 2.631

4.  A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509.

Authors:  James D Joseph; Nhin Lu; Jing Qian; John Sensintaffar; Gang Shao; Dan Brigham; Michael Moon; Edna Chow Maneval; Isan Chen; Beatrice Darimont; Jeffrey H Hager
Journal:  Cancer Discov       Date:  2013-06-18       Impact factor: 39.397

5.  An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).

Authors:  Manav Korpal; Joshua M Korn; Xueliang Gao; Daniel P Rakiec; David A Ruddy; Shivang Doshi; Jing Yuan; Steve G Kovats; Sunkyu Kim; Vesselina G Cooke; John E Monahan; Frank Stegmeier; Thomas M Roberts; William R Sellers; Wenlai Zhou; Ping Zhu
Journal:  Cancer Discov       Date:  2013-07-10       Impact factor: 39.397

6.  Emerging mechanisms of enzalutamide resistance in prostate cancer.

Authors:  Frank Claessens; Christine Helsen; Stefan Prekovic; Thomas Van den Broeck; Lien Spans; Hendrik Van Poppel; Steven Joniau
Journal:  Nat Rev Urol       Date:  2014-09-16       Impact factor: 14.432

7.  Glucocorticoid receptor confers resistance to antiandrogens by bypassing androgen receptor blockade.

Authors:  Vivek K Arora; Emily Schenkein; Rajmohan Murali; Sumit K Subudhi; John Wongvipat; Minna D Balbas; Neel Shah; Ling Cai; Eleni Efstathiou; Chris Logothetis; Deyou Zheng; Charles L Sawyers
Journal:  Cell       Date:  2013-12-05       Impact factor: 41.582

Review 8.  Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance.

Authors:  Xiaohong Tian; Yang He; Jinming Zhou
Journal:  Front Pharmacol       Date:  2015-03-24       Impact factor: 5.810

9.  Overcoming mutation-based resistance to antiandrogens with rational drug design.

Authors:  Minna D Balbas; Michael J Evans; David J Hosfield; John Wongvipat; Vivek K Arora; Philip A Watson; Yu Chen; Geoffrey L Greene; Yang Shen; Charles L Sawyers
Journal:  Elife       Date:  2013-04-09       Impact factor: 8.140

10.  Triptolide induces protective autophagy through activation of the CaMKKβ-AMPK signaling pathway in prostate cancer cells.

Authors:  Fei Zhao; Weiwei Huang; Zhe Zhang; Lin Mao; Yangyang Han; Jun Yan; Ming Lei
Journal:  Oncotarget       Date:  2016-02-02
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  1 in total

1.  A novel strategy to enhance terpenoids production using cambial meristematic cells of Tripterygium wilfordii Hook. f.

Authors:  Yadi Song; Shang Chen; Xiujuan Wang; Rui Zhang; Lichan Tu; Tianyuan Hu; Xihong Liu; Yifeng Zhang; Luqi Huang; Wei Gao
Journal:  Plant Methods       Date:  2019-11-07       Impact factor: 4.993
  1 in total

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