Geldanamycin
Application Notes
Geldanamycin is benzoquinone ansamycin antibiotic isolated from Streptomyces hygroscopicus. It is a potent antitumor metabolite that 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.
References
- Crystal structure of an Hsp90-geldanamycin complex: targeting of a chaperone by an antitumor agent. Stebbins C.E. et al., Cell 1997, 89, 239.
- Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90. Schneider C. et al., Proc Natl Acad Sci. USA 1996, 93, 14536.
- Preclinical evaluation of geldanamycin as an antitumor agent. Supko J.G et al., Cancer Chemother. Pharmacol. 1995, 36, 305.