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Overview
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17-Dimethylaminoethylamino-17-demethoxygeldanamycin (DMAG, alvespimycin) is a semi-synthetic derivative of the benzoquinone ansamycin antibiotic isolated from Streptomyces hygroscopicus in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group. DMAG acts by binding to the 90-kDa heat shock protein (Hsp90) essential to maintain the conformation, stability, activity and cellular localisation of several key oncogenic proteins such as ERBB2, C-RAF, CDK4, AKT/PKB, steroid hormone receptors, mutant p53, HIF-1α, survivin and telomerase hTERT. DMAG is more potent than geldanamycin and 17-allylamino-17-demethoxygeldanamycin (17AAG) as an inhibitor of Hsp90.
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