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Targeted Cancer Therapies

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There are several types of targeted therapies against specific...

Targeted Cancer Therapies

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Updated: May 30, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors

Published on: January 20, 2023

Heat shock proteins: a potential anticancer target.

Kamalesh K Sankhala¹, Monica M Mita, Alain C Mita

¹Institute for Drug Development at CTRC, The University of Texas Health Science Center, San Antonio, TX, USA. Sankhala@uthscsa.edu

Current Drug Targets

|July 23, 2011

Summary

This summary is machine-generated.

Heat shock protein 90 (Hsp90) inhibitors show promise as anticancer agents. Despite early toxicity concerns with geldanamycin, newer Hsp90 inhibitors are advancing in clinical trials for various cancers.

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Last Updated: May 30, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors

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Published on: January 20, 2023

Intracellular Refolding Assay

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Published on: January 24, 2012

Studies of Chaperone-Cochaperone Interactions using Homogenous Bead-Based Assay

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Published on: July 21, 2021

Area of Science:

Biochemistry
Molecular Biology
Oncology

Background:

Heat shock proteins (HSPs) are vital molecular chaperones crucial for cellular viability and stress response.
Hsp90 plays a key role in regulating proteins involved in cell proliferation, cell cycle control, angiogenesis, and apoptosis.
Hsp90's involvement in multiple oncogenic pathways makes it a significant target for cancer therapy.

Purpose of the Study:

To review the development and clinical potential of Heat shock protein 90 (Hsp90) inhibitors in cancer treatment.
To highlight the therapeutic promise of Hsp90 inhibitors as single agents or in combination therapies.

Main Methods:

Review of preclinical and clinical studies on Hsp90 inhibitors.
Analysis of the efficacy and safety profiles of various Hsp90 inhibitors, including geldanamycin and its successors.

Main Results:

Early Hsp90 inhibitor geldanamycin demonstrated anticancer activity but was limited by toxicity.
Subsequent generations of Hsp90 inhibitors exhibit improved safety profiles.
Clinical studies indicate promising anticancer activity in breast cancer, non-small cell lung carcinoma (NSCLC), gastrointestinal stromal tumors (GIST), and hematological malignancies.

Conclusions:

Hsp90 inhibitors represent a promising class of anticancer therapeutics.
The favorable safety profiles of newer inhibitors allow for exploration in clinical settings.
Hsp90 inhibitors are valuable candidates for both monotherapy and combination treatment strategies in oncology.