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Geldanamycin is a natural existing HSP90 (Heat Schock Protein 90) inhibitor, specifically disrupts glucocorticoid receptor (GR)/HSP association. The HSP90 chaperone is required for the activation of several families of eukaryotic protein kinases and nuclear hormone receptors, many of which are proto-oncogenic and play a prominent role in cancer.
Geldanamycin has antiproliferative and antitumor effects, as it binds to HSP90, inhibits the HSP90-mediated conformational maturation/refolding reaction. It interferes with cellular stress response. Geldanamycin decrease the expression of hypoxia inducible factor (HIF-1 alpha) in neural stem/progenitor cells.
Geldanomycin, U-29135, NSC 122750
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