In:
Biological Chemistry, Walter de Gruyter GmbH, Vol. 382, No. 3 ( 2001-03-21), p. 499-504
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.
Type of Medium:
Online Resource
ISSN:
1431-6730
Language:
Unknown
Publisher:
Walter de Gruyter GmbH
Publication Date:
2001
detail.hit.zdb_id:
1466062-3
SSG:
12