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 ◽  
...  
2008 ◽  
Vol 18 (7) ◽  
pp. 2495-2498 ◽  
Author(s):  
Christine Radanyi ◽  
Gaëlle Le Bras ◽  
Samir Messaoudi ◽  
Céline Bouclier ◽  
Jean-François Peyrat ◽  
...  

2001 ◽  
Vol 382 (3) ◽  
pp. 499-504 ◽  
Author(s):  
Marcus C. Rosenhagen ◽  
Jason C. Young ◽  
Gabriela M. Wochnik ◽  
Alexandra S. Herr ◽  
Ulrike Schmidt ◽  
...  

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.


2006 ◽  
Vol 5 (3) ◽  
pp. 522-532 ◽  
Author(s):  
Sharon Sanderson ◽  
Melanie Valenti ◽  
Sharon Gowan ◽  
Lisa Patterson ◽  
Zahida Ahmad ◽  
...  

2009 ◽  
Vol 52 (6) ◽  
pp. 1518-1521 ◽  
Author(s):  
Hugo G. Menzella ◽  
Thomas-Toan Tran ◽  
John R. Carney ◽  
Janice Lau-Wee ◽  
Jorge Galazzo ◽  
...  

2001 ◽  
Vol 120 (5) ◽  
pp. A357-A357
Author(s):  
T YOH ◽  
T NAKASHIMA ◽  
Y SUMIDA ◽  
Y KAKISAKA ◽  
H ISHIKAWA ◽  
...  

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