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Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
Update on Hsp90 inhibitors in clinical trial
1Medical Oncology Branch, NCI, NIH, Bethesda, MD 20892, USA.
Current Topics in Medicinal Chemistry
|October 29, 2009
Summary
Heat shock protein 90 (Hsp90) inhibitors show promise as anticancer drugs. Clinical trials are evaluating multiple Hsp90 inhibitors in adult and pediatric oncology, with ongoing development for improved efficacy.
Area of Science:
- Molecular Biology
- Oncology
- Pharmacology
Background:
- Heat shock protein 90 (Hsp90) is a crucial molecular chaperone implicated in cancer progression.
- Small molecule inhibitors targeting Hsp90 have been investigated for over two decades.
- Significant advancements have been made in understanding Hsp90's role in malignancy.
Purpose of the Study:
- To review the clinical trial results of Hsp90 inhibitors in cancer treatment.
- To discuss key challenges and future directions for developing Hsp90 inhibitors as anticancer therapeutics.
Main Methods:
- Review of clinical trial data for Hsp90 inhibitors.
- Analysis of progress in basic scientific understanding of Hsp90 chaperone machinery.
- Discussion of pivotal issues in the further development of Hsp90 inhibitors.
Main Results:
- The first Hsp90 inhibitor, 17-AAG, entered clinical trials in 1999.
- Currently, 13 distinct Hsp90 inhibitors are in clinical trials across various drug classes.
- Hundreds of patients, both adults and children, have been treated in oncology trials.
Conclusions:
- Hsp90 inhibitors represent a significant area of development in oncology.
- Clinical data thus far provides a basis for further therapeutic advancement.
- Addressing pivotal issues is crucial for the successful translation of Hsp90 inhibitors into effective anticancer drugs.
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