A Novel Mechanism of Androgen Receptor Action

2007 ◽  
Author(s):  
Jr Roberts ◽  
Charles T.
Keyword(s):  
Androgen Receptor ◽  
Receptor Action

scholarly journals Androgens and androgen receptor action in skin and hair follicles

2018 ◽  
Vol 465 ◽  
pp. 122-133 ◽  
Author(s):  
Julieta María Ceruti ◽  
Gustavo José Leirós ◽  
María Eugenia Balañá
Keyword(s):  
Androgen Receptor ◽  
Hair Follicles ◽  
Receptor Action

scholarly journals Small Molecule Inhibitors as Probes for Estrogen and Androgen Receptor Action

2010 ◽  
Vol 286 (6) ◽  
pp. 4043-4048 ◽  
Author(s):  
David J. Shapiro ◽  
Chengjian Mao ◽  
Milu T. Cherian
Keyword(s):  
Androgen Receptor ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Receptor Action

scholarly journals BAP18 coactivates androgen receptor action and promotes prostate cancer progression

2016 ◽  
Vol 44 (17) ◽  
pp. 8112-8128 ◽  
Author(s):  
Shiying Sun ◽  
Xinping Zhong ◽  
Chunyu Wang ◽  
Hongmiao Sun ◽  
Shengli Wang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Cancer Progression ◽  
Prostate Cancer Progression ◽  
Receptor Action

scholarly journals Differential Modulation of Androgen Receptor Action by Deoxyribonucleic Acid Response Elements

2003 ◽  
Vol 17 (9) ◽  
pp. 1738-1750 ◽  
Author(s):  
Christoph Geserick ◽  
Hellmuth-Alexander Meyer ◽  
Karina Barbulescu ◽  
Bernard Haendler
Keyword(s):  
Androgen Receptor ◽  
Deoxyribonucleic Acid ◽  
Differential Modulation ◽  
Response Elements ◽  
Receptor Action

Abstract 1581: Androgen receptor action in prostate cancer partitions into distinct transcriptional codes that differ in clinical relevance

2017 ◽  
Author(s):  
Sangeeta Kumari ◽  
Varadha Balaji Venkadakrishnan ◽  
Dhirodatta Senapati ◽  
Qiang Hu ◽  
Song Liu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Clinical Relevance ◽  
Receptor Action

scholarly journals Sex Hormone-Binding Globulin Mediates Prostate Androgen Receptor Action via a Novel Signaling Pathway

Endocrinology ◽  
1998 ◽  
Vol 139 (1) ◽  
pp. 213-218 ◽  
Author(s):  
Victor D. H. Ding ◽  
David E. Moller ◽  
William P. Feeney ◽  
Varsha Didolkar ◽  
Atif M. Nakhla ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Signaling Pathway ◽  
Sex Hormone ◽  
Sex Hormone Binding Globulin ◽  
Hormone Binding ◽  
Receptor Action

Mechanism of androgen receptor action

Maturitas ◽  
2009 ◽  
Vol 63 (2) ◽  
pp. 142-148 ◽  
Author(s):  
Jin Li ◽  
Farook Al-Azzawi
Keyword(s):  
Androgen Receptor ◽  
Receptor Action

scholarly journals Differential modulation of androgen receptor transcriptional activity by the nuclear receptor co-repressor (N-CoR)

2004 ◽  
Vol 379 (3) ◽  
pp. 731-738 ◽  
Author(s):  
Cor A. BERREVOETS ◽  
Arzu UMAR ◽  
Jan TRAPMAN ◽  
Albert O. BRINKMANN
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Conformational Change ◽  
Nuclear Receptor ◽  
Cyproterone Acetate ◽  
Transcriptional Activity ◽  
Differential Modulation ◽  
Partial Agonists ◽  
Receptor Action

Antiandrogens are widely used agents in the treatment of prostate cancer, as inhibitors of AR (androgen receptor) action. Although the precise mechanism of antiandrogen action is not yet elucidated, recent studies indicate the involvement of nuclear receptor co-repressors. In the present study, the regulation of AR transcriptional activity by N-CoR (nuclear receptor co-repressor), in the presence of different ligands, has been investigated. Increasing levels of N-CoR differentially affected the transcriptional activity of AR occupied with either agonistic or antagonistic ligands. Small amounts of co-transfected N-CoR repressed CPA (cyproterone acetate)- and mifepristone (RU486)-mediated AR activity, but did not affect agonist (R1881)-induced AR activity. Larger amounts of co-transfected N-CoR repressed AR activity for all ligands, and converted the partial agonists CPA and RU486 into strong AR antagonists. In the presence of the agonist R1881, co-expression of the p160 co-activator TIF2 (transcriptional intermediary factor 2) relieved N-CoR repression up to control levels. However, in the presence of RU486 and CPA, TIF2 did not functionally compete with N-CoR, suggesting that antagonist-bound AR has a preference for N-CoR. The AR mutation T877A (Thr877→Ala), which is frequently found in prostate cancer and affects the ligand-induced conformational change of the AR, considerably reduced the repressive action of N-CoR. The agonistic activities of CPA- and hydroxyflutamide-occupied T877A-AR were hardly affected by N-CoR, whereas TIF2 strongly enhanced their activities. These results indicate that lack of N-CoR action allows these antiandrogens to act as strong agonists on the mutant AR.

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