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.
Keywords: 17AAG, 17DMAG, PU-class Hsp90 inhibitors, radicicol and derivatives, 3,4-diarylpyrazoles, anti-cancer therapeutics
Anti-Cancer Agents in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/187152006774755483 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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