Abstract
Hsp90 is involved in the maturation and activation of client proteins. Often these are key proteins involved in signal transduction and regulatory pathways that in a mutated and/or deregulated form sustain an oncogenic cellular state. Consequently, the malignancy is maintained with the aid of Hsp90 upon which the mutated proteins have become particularly dependent for their activity. The requirement for the Hsp90 chaperone machine to drive the malignancy makes Hsp90 a prime anticancer target, an ‘axle in a wheel’ that when disrupted has been shown to be effective in killing cancerous cells. This review aims to identify potential drug targets, based on the current structural knowledge of the Hsp90-chaperone machine, that could be targeted with the aim of disrupting its functioning and promoting an anti-cancer activity.
Keywords: Heat shock protein, Hsp90, co-chaperones, cancer, drug design
Current Topics in Medicinal Chemistry
Title: Strategies for Stalling Malignancy: Targeting Cancers Addiction to Hsp90
Volume: 9 Issue: 15
Author(s): Chrisostomos Prodromou
Affiliation:
Keywords: Heat shock protein, Hsp90, co-chaperones, cancer, drug design
Abstract: Hsp90 is involved in the maturation and activation of client proteins. Often these are key proteins involved in signal transduction and regulatory pathways that in a mutated and/or deregulated form sustain an oncogenic cellular state. Consequently, the malignancy is maintained with the aid of Hsp90 upon which the mutated proteins have become particularly dependent for their activity. The requirement for the Hsp90 chaperone machine to drive the malignancy makes Hsp90 a prime anticancer target, an ‘axle in a wheel’ that when disrupted has been shown to be effective in killing cancerous cells. This review aims to identify potential drug targets, based on the current structural knowledge of the Hsp90-chaperone machine, that could be targeted with the aim of disrupting its functioning and promoting an anti-cancer activity.
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Cite this article as:
Prodromou Chrisostomos, Strategies for Stalling Malignancy: Targeting Cancers Addiction to Hsp90, Current Topics in Medicinal Chemistry 2009; 9 (15) . https://dx.doi.org/10.2174/156802609789895656
DOI https://dx.doi.org/10.2174/156802609789895656 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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