Geldanamycin from Streptomyces hygroscopicus

For R&D use onlynot for drug household or other uses.

Geldanamycin is a 14-benzoquinone ansamycin antitumor antibiotic that inhibits the function of Hsp90 (Heat Shock Protein 90) by binding to the unusual ADPATP-binding pocket of the protein. HSP90 client proteins play important roles in the regulation of the cell cycle cell growth cell survival apoptosis angiogenesis and oncogenesis.Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential geldanamycin presents several major drawbacks as a drug candidate such as hepatotoxicity further Jilani et al. reported that geldanamycin induces the apoptosis of erythrocytes under physiological concentrations. These side effects have led to the development of geldanamycin analogues in particular analogues containing a derivatisation at the 17 position