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Updated: May 15, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
HSP90 inhibitors: current development and potential in cancer therapy
Katerina Sidera, Evangelia Patsavoudi1
1Dept. of Biochemistry, Hellenic Pasteur Institute, 127, Vas. Sofias Av., 11521 Athens, Greece. epatsavoudi@pasteur.gr.
Abstract:
In the last decade, the molecular chaperone HSP90 has emerged as an important target in cancer therapeutics and has subsequently become the focus of several drug discovery and development efforts. The first-in-class HSP90 inhibitor 17-AAG entered into Phase I clinical trial in 1999. Today 13 HSP90 inhibitors representing multiple drug classes, with different modes of action, are undergoing clinical evaluation. The present review will highlight the involvement of HSP90 in regulating and maintaining the transformed phenotype, provide an overview on current HSP90 inhibitors and further update on the most relevant patents which have recently appeared in the literature.
Insights
Heat shock protein 90 (HSP90) is a key target in cancer therapy. Numerous HSP90 inhibitors are now in clinical trials, with ongoing drug discovery and patent activity.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- The molecular chaperone HSP90 plays a critical role in maintaining the transformed phenotype of cancer cells.
- HSP90 is recognized as a significant therapeutic target in oncology.
- Extensive drug discovery efforts have focused on HSP90 inhibitors.
Purpose of the Study:
- To review the role of HSP90 in cancer.
- To provide an overview of current HSP90 inhibitors in clinical development.
- To update on recent patents related to HSP90 inhibitors.
Main Methods:
- Literature review of HSP90's role in cancer.
- Survey of clinical trial data for HSP90 inhibitors.
- Analysis of recent patent filings for HSP90-targeting drugs.
Main Results:
- HSP90 is crucial for cancer cell survival and proliferation.
- Thirteen HSP90 inhibitors across various drug classes are in clinical evaluation.
- Significant patent activity indicates continued innovation in HSP90 inhibitor development.
Conclusions:
- HSP90 remains a promising target for cancer therapeutics.
- The diverse range of inhibitors and ongoing research highlight the therapeutic potential.
- Further development and clinical evaluation of HSP90 inhibitors are warranted.
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