Document Detail

Ligand-independent androgen receptor antagonism caused by the newly developed pesticide pyrifluquinazon (PFQ).
MedLine Citation:
PMID:  23146716     Owner:  NLM     Status:  Publisher    
Androgen receptor (AR) is an essential component to activate AR dependent gene transcriptions. Despite wide acceptance of pharmacological controls on transcriptional pathway depending on competitive inhibitions of ligand binding, only a few examples, AR antagonism via ligand-independent mechanisms, have been recognized. Pyrifluquinazon(PFQ), a newly developed pesticide, induced representative AR antagonism against rats in in vivo and in vitro. Intriguingly, this AR antagonism was not based on inhibition of ligand binding. Instead, the evidence suggested that the AR antagonism was induced as a consequence of decline of cellular AR protein level. This study demonstrated that AR N-terminal region could be an essential element for a ligand-independent mechanism underling the AR antagonism by PFQ. Our findings should provide a novel insight into the regulation of AR-mediated transcription.
Ryoko Yasunaga; Junko Ikuta; Yohei Murata; Kazuyoshi Inoue; Hiroyasu Koga; Takao Masaki; Hiroto Tamura
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-9
Journal Detail:
Title:  Reproductive toxicology (Elmsford, N.Y.)     Volume:  -     ISSN:  1873-1708     ISO Abbreviation:  Reprod. Toxicol.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-13     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8803591     Medline TA:  Reprod Toxicol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012. Published by Elsevier Inc.
Research and Development Division, Nihon Nohyaku Co. Ltd., 345 Oyamada-cho, Kawachi-nagano, Osaka 586-0094, Japan.
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