17-allylamino-17-demethoxygeldanamycin (17-AAG), a semi-synthetic derivative of geldanamycin, is a potent antitumor agent 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. 17-AAG increases the sensitivity of pediatric acute lymphoblastic leukemia cell lines with varying Bcr-Abl status to imatinib in vitro.
Hawkins LM et al (2005) Effects of 17-allylamino-17-demethoxygeldanamycin (17-AAG) on pediatric acute lymphoblastic leukemia (ALL) with respect to Bcr-Abl status and imatinib mesylate sensitivity. Pediatr. Res. 57:43
Schneider C. et al. (1996) Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90. Proc. Nat.l Acad. Sci. USA 93:14536
Villa R. et al. (2003) Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells. Carcinogenesis 24:851