scholarly journals Enzymatic Reduction and Glutathione Conjugation of Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors: Relevance for Toxicity and Mechanism of Action

2008 ◽  
Vol 36 (10) ◽  
pp. 2050-2057 ◽  
Author(s):  
Wenchang Guo ◽  
Philip Reigan ◽  
David Siegel ◽  
David Ross
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Mechanism Of Action ◽  
Heat Shock Protein 90 ◽  
Glutathione Conjugation ◽  
Enzymatic Reduction ◽  
Benzoquinone Ansamycin

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

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.

Benzoquinone ansamycin heat shock protein 90 inhibitors modulate multiple functions required for tumor angiogenesis

2006 ◽  
Vol 5 (3) ◽  
pp. 522-532 ◽  
Author(s):  
Sharon Sanderson ◽  
Melanie Valenti ◽  
Sharon Gowan ◽  
Lisa Patterson ◽  
Zahida Ahmad ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Tumor Angiogenesis ◽  
Heat Shock Protein 90 ◽  
Multiple Functions ◽  
Benzoquinone Ansamycin

Potent Non-Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors from Genetic Engineering ofStreptomyces hygroscopicus

2009 ◽  
Vol 52 (6) ◽  
pp. 1518-1521 ◽  
Author(s):  
Hugo G. Menzella ◽  
Thomas-Toan Tran ◽  
John R. Carney ◽  
Janice Lau-Wee ◽  
Jorge Galazzo ◽  
...  
Keyword(s):  
Heat Shock ◽  
Genetic Engineering ◽  
Heat Shock Protein ◽  
Heat Shock Protein 90 ◽  
Benzoquinone Ansamycin

Glycyrrhizin effects rat hepatocytes via the reduction of heat shock protein 90 expression

2001 ◽  
Vol 120 (5) ◽  
pp. A357-A357
Author(s):  
T YOH ◽  
T NAKASHIMA ◽  
Y SUMIDA ◽  
Y KAKISAKA ◽  
H ISHIKAWA ◽  
...  
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Heat Shock Protein 90 ◽  
Rat Hepatocytes
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