Geldanamycin, a Heat Shock Protein 90-Binding Benzoquinone Ansamycin, Inhibits Steroid-Dependent Translocation of the Glucocorticoid Receptor from the Cytoplasm to the Nucleus†

Biochemistry ◽  
1997 ◽  
Vol 36 (25) ◽  
pp. 7776-7785 ◽  
Author(s):  
Michael J. Czar ◽  
Mario D. Galigniana ◽  
Adam M. Silverstein ◽  
William B. Pratt
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Glucocorticoid Receptor ◽  
Heat Shock Protein 90 ◽  
Steroid Dependent ◽  
Benzoquinone Ansamycin

Synergistic Inhibition of the Glucocorticoid Receptor by Radicicol and Benzoquinone Ansamycins

2001 ◽  
Vol 382 (3) ◽  
pp. 499-504 ◽  
Author(s):  
Marcus C. Rosenhagen ◽  
Jason C. Young ◽  
Gabriela M. Wochnik ◽  
Alexandra S. Herr ◽  
Ulrike Schmidt ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Glucocorticoid Receptor ◽  
Nuclear Receptors ◽  
Therapeutic Target ◽  
Heat Shock Protein 90 ◽  
Model System ◽  
Hormone Binding ◽  
Synergistic Inhibition ◽  
Benzoquinone Ansamycin

Abstract Radicicol (RAD) and the benzoquinone ansamycin geldanamycin (GA) are potential anticancer drugs known to inhibit heat shock protein 90 (hsp90) and, therefore, the activation of proteins dependent on its function such as protooncogenic kinases and nuclear receptors. Using the glucocorticoid receptor (GR) as a model system we analysed the effects of RAD and various benzoquinone ansamycins. All compounds efficiently abolished GRdependent transactivation. Surprisingly, whenever one of the ansamycins was applied in combination with RAD, synergistic inhibition of GRdependent transcription and of hormone binding of GR was observed. In contrast, combination of two ansamycins showed no synergy. These findings suggest synergism within the hsp90 dimer and may open new ways to explore hsp90 as therapeutic target.

scholarly journals 19-Substituted Benzoquinone Ansamycin Heat Shock Protein-90 Inhibitors: Biological Activity and Decreased Off-Target Toxicity

2014 ◽  
Vol 85 (6) ◽  
pp. 849-857 ◽  
Author(s):  
Chuan-Hsin Chang ◽  
Derek A. Drechsel ◽  
Russell R. A. Kitson ◽  
David Siegel ◽  
Qiang You ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heat Shock ◽  
Heat Shock Protein ◽  
Heat Shock Protein 90 ◽  
Benzoquinone Ansamycin

Interaction of glucocorticoid receptor with heat shock protein 90 after chronic stress

1996 ◽  
Vol 6 ◽  
pp. 110
Author(s):  
Y. Sasuga ◽  
M. Asakura ◽  
M. Miyamoto ◽  
N. Bodaiji ◽  
J. Imafuku ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Glucocorticoid Receptor ◽  
Chronic Stress ◽  
Heat Shock Protein 90

scholarly journals Heat Shock Protein 90-Dependent (Geldanamycin-Inhibited) Movement of the Glucocorticoid Receptor through the Cytoplasm to the Nucleus Requires Intact Cytoskeleton

1998 ◽  
Vol 12 (12) ◽  
pp. 1903-1913 ◽  
Author(s):  
Mario D. Galigniana ◽  
Jennifer L. Scruggs ◽  
James Herrington ◽  
Michael J. Welsh ◽  
Christin Carter-Su ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Glucocorticoid Receptor ◽  
Heat Shock Protein 90

Differential Alteration of Heat Shock Protein 90 in Mice Modifies Glucocorticoid Receptor Function and Susceptibility to Trauma

2010 ◽  
Vol 27 (2) ◽  
pp. 373-381 ◽  
Author(s):  
Hai-Ying Shen ◽  
Yan Zhao ◽  
Xing-Yun Chen ◽  
Ren-Ping Xiong ◽  
Jin-Li Lu ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Glucocorticoid Receptor ◽  
Heat Shock Protein 90 ◽  
Receptor Function
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