scholarly journals Structure−Activity Relationship for Thiohydantoin Androgen Receptor Antagonists for Castration-Resistant Prostate Cancer (CRPC)

2010 ◽  
Vol 53 (7) ◽  
pp. 2779-2796 ◽  
Author(s):  
Michael E. Jung ◽  
Samedy Ouk ◽  
Dongwon Yoo ◽  
Charles L. Sawyers ◽  
Charlie Chen ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Castration Resistant Prostate Cancer ◽  
Receptor Antagonists ◽  
Castration Resistant ◽  
Structure Activity ◽  
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

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.

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