Mechanism of Antiandrogen Action: Key Role of Hsp90 in Conformational Change and Transcriptional Activity of the Androgen Receptor

Activation of the androgen receptor (AR) is induced by ligand binding through conformational changes leading to control of gene expression. Antiandrogens compete with androgens for AR occupancy and subsequently block at least one step in AR action. Analysis of nuclear transfer kinetics using the GFP...

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Veröffentlicht in:	Biochemistry (Easton) 2002-10, Vol.41 (39), p.11824-11831
Hauptverfasser:	Georget, Virginie, Térouanne, Béatrice, Nicolas, Jean-Claude, Sultan, Charles
Format:	Artikel
Sprache:	eng
Schlagworte:	Active Transport, Cell Nucleus - drug effects Active Transport, Cell Nucleus - genetics Androgen Antagonists - chemistry Androgen Antagonists - pharmacology Animals Benzoquinones Cell Line Cell Nucleus - chemistry Cell Nucleus - drug effects Cell Nucleus - genetics COS Cells Endopeptidases Green Fluorescent Proteins HSP90 Heat-Shock Proteins - antagonists & inhibitors HSP90 Heat-Shock Proteins - physiology Humans Hydrolysis Kinetics Lactams, Macrocyclic Luminescent Proteins - genetics Microscopy, Fluorescence Plasmids Protein Conformation Quinones - pharmacology Receptors, Androgen - chemistry Receptors, Androgen - genetics Receptors, Androgen - physiology Trans-Activators - chemistry Trans-Activators - genetics Trans-Activators - physiology Transfection
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