Chemical Name:9,13-Dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethy
l-2-azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20
,22-trione, 9-carbamate
Biological Activity:
Selectively inhibits heat shock
protein 90 (Hsp90). Binds to the ATP site of Hsp90 (Kd = 1.2 μM)
and inhibits its chaperone activity. Consequently inhibits activities of
oncogenic kinases (e.g. src, Raf), p53 and steroid receptors.
Whitesellet al (1994) Inhibition of heat shock protein
HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins:
essential role for stress proteins in oncogenic transformation.
Proc.Natl.Acad.Sci.USA 91 8324. Cardenaset al
(1998) Signal-transduction cascades as targets for therapeutic intervention by
natural products. TiBTECH 16 427. Roeet al (1999)
Structural basis for inhibition of the Hsp90 molecular chaperone by the
antitumor antibiotics radicicol and geldanomycin. J.Med.Chem. 42
260.
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