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Updated: Mar 29, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
Heat shock protein 90 targeting therapy: state of the art and future perspective
Manabu Tatokoro1, Fumitaka Koga2, Soichiro Yoshida1
1Department of Urology, Tokyo Medical and Dental University Graduate School, Tokyo, Japan.
Abstract:
Heat shock protein 90 (Hsp90) is an ATP-dependent molecular chaperone that plays a role in stabilizing and activating more than 200 client proteins. It is required for the stability and function of numerous oncogenic signaling proteins that determine the hallmarks of cancer. Since the initial discovery of the first Hsp90 inhibitor in the 1970s, multiple phase II and III clinical trials of several Hsp90 inhibitors have been undertaken. This review provides an overview of the current status on clinical trials of Hsp90 inhibitors and future perspectives on novel anticancer strategies using Hsp90 inhibitors.
Insights
Heat shock protein 90 (Hsp90) is crucial for cancer protein stability. This review details Hsp90 inhibitor clinical trials and future anticancer strategies.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Heat shock protein 90 (Hsp90) is a molecular chaperone essential for stabilizing over 200 client proteins.
- Hsp90 is vital for the function of numerous oncogenic signaling proteins, contributing to cancer hallmarks.
- The development of Hsp90 inhibitors has been pursued since the 1970s.
Purpose of the Study:
- To provide an overview of the current clinical trial status of Hsp90 inhibitors.
- To discuss future perspectives for novel anticancer strategies utilizing Hsp90 inhibitors.
Main Methods:
- Review of existing literature on Hsp90 inhibitors.
- Analysis of data from Phase II and III clinical trials.
- Exploration of emerging therapeutic approaches targeting Hsp90.
Main Results:
- Multiple Hsp90 inhibitors have advanced to Phase II and III clinical trials.
- Significant research efforts are ongoing to develop Hsp90-targeted cancer therapies.
- Hsp90 inhibition represents a promising avenue for novel anticancer drug development.
Conclusions:
- Hsp90 inhibitors are a key focus in ongoing cancer research and clinical development.
- Further investigation into Hsp90-targeted strategies holds potential for advancing cancer treatment.
- The review highlights the evolving landscape of Hsp90 inhibitor-based anticancer therapies.
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