Molecular chaperone Hsp90 as a target for oxidant-based anticancer therapies
R Beck1, N Dejeans, C Glorieux
1Toxicology and Cancer Biology Research Group, Louvain Drug Research Institute, Université Catholique de Louvain, Belgium.
Abstract:
Hsp90 is a molecular chaperone involved in the stabilization of many oncoproteins that are required for the acquisition and maintenance of the so-called six major hallmarks of cancer cells. Various strategies have, therefore, been developed to inhibit the chaperone activity of Hsp90 and induce cancer cell death through the destabilization of its client proteins. Among these strategies, we have shown that generation of oxidative stress leads to the cleavage and deactivation of Hsp90. Because cancer cells are often deficient in antioxidant enzymes and exhibit higher basal levels of reactive oxygen species (ROS) than their normal counterparts, inducing a selective oxidative stress may be a promising approach for cancer treatment. Thus, many redox-modulating agents have, therefore, been developed or are undergoing clinical trials and Hsp90 represents a new target for oxidative stress-generating agents. The purpose of this article is to review the current state of knowledge about Hsp90 and the use of oxidative stress-generating agents in cancer treatment. We will illustrate the review with some of our results concerning the effects of oxidative stress on Hsp90 using various oxidative stress-generating systems based on different quinones in combination with a well-known reducing agent (i.e., ascorbate). Our results show that oxidative stress provokes the cleavage of Hsp90 in CML cells, as well as the degradation of its client protein Bcr-Abl and the deactivation of its downstream signaling pathways, namely MAPK and STAT5. Overall, these results highlight the potential interest of using oxidative stress to target Hsp90.
Insights
Targeting heat shock protein 90 (Hsp90) with oxidative stress shows promise for cancer treatment. Inducing oxidative stress cleaves Hsp90, leading to cancer cell death by destabilizing key oncoproteins.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Heat shock protein 90 (Hsp90) stabilizes oncoproteins crucial for cancer hallmarks.
- Inhibiting Hsp90 can induce cancer cell death by destabilizing its client proteins.
- Cancer cells often have heightened reactive oxygen species (ROS) levels and reduced antioxidant capacity.
Purpose of the Study:
- To review the role of Hsp90 in cancer.
- To explore the potential of oxidative stress-generating agents in targeting Hsp90 for cancer therapy.
- To present findings on oxidative stress-induced Hsp90 cleavage and its downstream effects.
Main Methods:
- Review of current literature on Hsp90 and oxidative stress in cancer.
- Experimental investigation using quinone-based oxidative stress systems and ascorbate.
- Analysis of Hsp90 cleavage, client protein degradation (Bcr-Abl), and signaling pathway activity (MAPK, STAT5) in CML cells.
Main Results:
- Oxidative stress induces Hsp90 cleavage and deactivation in chronic myeloid leukemia (CML) cells.
- Hsp90 client protein Bcr-Abl is degraded following oxidative stress.
- Downstream signaling pathways (MAPK, STAT5) are deactivated, contributing to cancer cell death.
Conclusions:
- Targeting Hsp90 with oxidative stress is a promising strategy for cancer treatment.
- Selective induction of oxidative stress can exploit cancer cell vulnerabilities.
- This approach offers a novel therapeutic avenue by disrupting critical cancer-promoting pathways.
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