scholarly journals Androgen Receptor Antagonists in Castration-Resistant Prostate Cancer

2013 ◽  
Vol 19 (1) ◽  
pp. 43-49 ◽  
Author(s):  
Dana Rathkopf ◽  
Howard I. Scher
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Castration Resistant Prostate Cancer ◽  
Receptor Antagonists ◽  
Castration Resistant ◽  
Androgen Receptor Antagonists

scholarly journals In Silico Discovery of Androgen Receptor Antagonists with Activity in Castration Resistant Prostate Cancer

2012 ◽  
Vol 26 (11) ◽  
pp. 1836-1846 ◽  
Author(s):  
Howard C. Shen ◽  
Kumaran Shanmugasundaram ◽  
Nicholas I. Simon ◽  
Changmeng Cai ◽  
Hongyun Wang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
In Silico ◽  
Castration Resistant Prostate Cancer ◽  
Receptor Antagonists ◽  
Castration Resistant ◽  
Androgen Receptor Antagonists

scholarly journals PD59-08 COMBINATION THERAPY WITH NOVEL ANDROGEN RECEPTOR ANTAGONISTS AND STATIN FOR CASTRATION-RESISTANT PROSTATE CANCER

2020 ◽  
Vol 203 ◽  
pp. e1207-e1208
Author(s):  
Hiroshi Nakayama* ◽  
Yoshitaka Sekine ◽  
Daisuke Oka ◽  
Masanori Aoki ◽  
Akira Ohtsu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Combination Therapy ◽  
Castration Resistant Prostate Cancer ◽  
Receptor Antagonists ◽  
Castration Resistant ◽  
Androgen Receptor Antagonists

Non-Steroidal Androgen Receptor Antagonists and Prostate Cancer: A Survey on Chemical Structures Binding this Fast-Mutating Target

2019 ◽  
Vol 26 (33) ◽  
pp. 6053-6073 ◽  
Author(s):  
Claudia Ferroni ◽  
Greta Varchi
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Small Molecules ◽  
Molecular Target ◽  
Selective Inhibitor ◽  
Castration Resistant Prostate Cancer ◽  
Receptor Antagonists ◽  
Chemical Structures ◽  
Castration Resistant ◽  
Androgen Receptor Antagonists

The Androgen Receptor (AR) pathway plays a major role in both the pathogenesis and progression of prostate cancer. In particular, AR is chiefly involved in the development of Castration-Resistant Prostate Cancer (CRPC) as well as in the resistance to the secondgeneration AR antagonist enzalutamide, and to the selective inhibitor of cytochrome P450 17A1 (CYP17A1) abiraterone. Several small molecules acting as AR antagonists have been designed and developed so far, also as a result of the ability of cells expressing this molecular target to rapidly develop resistance and turn pure receptor antagonists into ineffective or event detrimental molecules. This review covers a survey of most promising classes of non-steroidal androgen receptor antagonists, also providing insights into their mechanism of action and efficacy in treating prostate cancer.

Degradation of Androgen Receptor through Small Molecules for Prostate Cancer

2018 ◽  
Vol 18 (7) ◽  
pp. 652-667 ◽  
Author(s):  
Raoling Ge ◽  
Xi Xu ◽  
Pengfei Xu ◽  
Lei Li ◽  
Zhiyu Li ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Small Molecules ◽  
Androgen Deprivation Therapy ◽  
Resistance Mechanism ◽  
Androgen Deprivation ◽  
High Expression ◽  
Castration Resistant Prostate Cancer ◽  
Castration Resistant ◽  
Androgen Receptor Antagonists

Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen receptor converts the action of enzalutamide and ARN-509 from an antagonist to agonist, so that novel strategies are urgent to address this resistance mechanism. In this review, we focus on the discussion about some novel strategies, which targets androgen receptor mainly through the degrading pathway as potential treatments for prostate cancer.

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