Emerging Hsp90 Inhibitors: From Discovery to Clinic

Title: Emerging Hsp90 Inhibitors: From Discovery to Clinic

Volume: 6 Issue: 1

Author(s): G. Chiosis, A. Rodina and K. Moulick

Affiliation:

Keywords: 17AAG, 17DMAG, PU-class Hsp90 inhibitors, radicicol and derivatives, 3,4-diarylpyrazoles, anti-cancer therapeutics

Abstract: Hsp90 is a chaperone with important roles in maintaining transformation and in elevating the survival and growth potential of cancer cells. Activation of signaling pathways mediated by Hsp90 protein clients is necessary for cell proliferation, regulation of cell cycle progression and apoptosis. Additionally, gain-of-function mutations responsible for transformation often require Hsp90 for the maintenance of their folded, functionally active conformations. These characteristics promise Hsp90 as an important target in cancer therapy and prompt for the identification, development and clinical translation of small molecule inhibitors of the chaperone. This review intends to update the reader on the status of several existing and emerging classes of direct inhibitors of Hsp90 ATPase activity.

Cite this article as:

Chiosis G., Rodina A. and Moulick K., Emerging Hsp90 Inhibitors: From Discovery to Clinic, Anti-Cancer Agents in Medicinal Chemistry 2006; 6 (1) . https://dx.doi.org/10.2174/187152006774755483