Rapid paperMechanism of antiandrogen action: Conformational changes of the receptor
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2020, Asian Journal of UrologyCitation Excerpt :The reason why the AR-LBD crystal structure could not be resolved and what is unique about the AR-LBD that prevents its structural elucidation, remains important unanswered questions. The only information that is currently available comes from limited trypsinization studies and cofactor-interaction profiling that indicate that the AR conformation in the presence of agonists and antagonists is distinct [79,80]. Similar to the other hormone receptor LBD domains, AR-LBD is also comprised of an α-helical structure.
Reproductive and nonreproductive actions of testosterone
2018, Encyclopedia of Endocrine DiseasesDesign, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists
2015, European Journal of Medicinal ChemistryCitation Excerpt :In many cases the resistance is strongly associated with the pull of point mutations occurred predominantly in androgen binding site leading to the aberrant receptor up-regulation and higher sensitivity rather than down-regulation and relaxation upon antiandrogen therapy. It should be noted that AR agonists and AR antagonists share different modes of action towards the related transcriptional machinery inducing the “closed” and “open” conformations of AR-H12 helix [17–19]. Therefore, even minor modifications in the structure of a small molecule AR ligand can lead to dramatic alterations in the receptor–ligand interaction thereby providing opposite pharmacological responses.
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2015, Endocrine Disruption and Human Health