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Radicicol, also known as monorden, is a
fungal resorcylic acid lactone and natural-product
HSP90 inhibitor. It binds the N-terminal ATP-binding pocket
of HSP90 and inhibits its molecular-chaperone activity, resulting in
destabilization and degradation of HSP90-dependent client proteins involved
in tumour growth and survival. Reported effects include suppression of
oncogenic kinase signalling, cell-cycle arrest, and apoptosis in experimental
cancer models. Although radicicol is potent in biochemical and cell-based
assays, the native compound has limited therapeutic utility because of
chemical instability, rapid metabolism, and weak in-vivo activity.
Reference.
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