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Updated: Sep 14, 2025

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

Published on: January 20, 2023

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Recent advances in HSP90 inhibitors as targeted cancer therapy: Chemical scaffolds, isoform selectivity, and clinical

Bharat Goel1, Shivani Jaiswal2, Nancy Tripathi3

  • 1Amity School of Pharmaceutical Sciences, Amity University Punjab, Mohali 140306, India.

Bioorganic Chemistry
|July 24, 2025
PubMed

Insights

Heat shock protein 90 (HSP90) inhibitors show promise in cancer therapy by targeting key oncoproteins. Recent advancements focus on developing novel small molecules and natural products to overcome challenges in clinical translation.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Heat shock protein 90 (HSP90) is crucial for stabilizing oncoproteins driving cancer growth.
  • HSP90 overexpression is common in various cancers, contributing to metastasis and treatment resistance.
  • Targeting HSP90 offers a therapeutic strategy against multiple cancer types.

Purpose of the Study:

  • To review recent (2020-2024) progress in HSP90 inhibitor discovery and development.
  • To summarize advancements in medicinal chemistry and chemical biology of HSP90 inhibitors.
  • To discuss preclinical and clinical development, and challenges in translating HSP90 inhibitors into cancer therapies.

Main Methods:

  • Comprehensive literature review of HSP90 inhibitor research from 2020-2024.
  • Analysis of natural products and synthetic small molecules targeting HSP90.
  • Evaluation of preclinical and clinical trial data for HSP90 inhibitors.

Main Results:

  • Significant progress in medicinal chemistry and chemical biology of HSP90 inhibitors.
  • Development of novel small molecules and natural product-derived compounds.
  • Variable efficacy and tolerability profiles observed for ongoing clinical trials.

Conclusions:

  • HSP90 remains a validated target for anticancer drug development.
  • Continued research is needed to optimize HSP90 inhibitors for improved clinical outcomes.
  • Overcoming challenges in efficacy and tolerability is key for successful translation.
Keywords:
AnticancerChaperoneClient proteinsClinical trialsHSP90Natural products

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