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Updated: Mar 3, 2026

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
BIIB021: A novel inhibitor to heat shock protein 90-addicted oncology
Liang Yan1, Weiming Zhang2, Beibei Zhang3
11 Department of Oncology, Binzhou People's Hospital, Binzhou, People's Republic of China.
Abstract:
Heat shock protein 90 is induced in response to the cell stress. Its overexpression has been reported in many cancers with poor prognosis. It acts as a chaperone to the client proteins, especially the activated oncoproteins in malignancies to protect them from degradation. Heat shock protein 90 inhibition represented anti-cancer effects in many studies. Previous natural product-based compounds are limited by their association with target toxicities. BIIB021 is an orally available, fully synthetic novel small-molecule heat shock protein 90 inhibitor that has shown strong antitumor activities in a large number of preclinical models and is now under clinical investigation. This review will summarize its therapeutic effects and highlight the prospect of targeting heat shock protein 90 in the cancer therapy.
Insights
Heat shock protein 90 (HSP90) is a cancer target. The novel inhibitor BIIB021 shows strong antitumor effects in preclinical models and is under clinical investigation for cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Heat shock protein 90 (HSP90) is upregulated in various cancers, correlating with poor prognosis.
- HSP90 functions as a molecular chaperone, stabilizing oncoproteins and preventing their degradation.
- Inhibition of HSP90 has demonstrated anti-cancer effects, but natural product inhibitors face toxicity limitations.
Purpose of the Study:
- To review the therapeutic effects of BIIB021, a novel small-molecule HSP90 inhibitor.
- To highlight the potential of targeting HSP90 in cancer treatment strategies.
Main Methods:
- Review of preclinical data and clinical investigation of BIIB021.
- Summary of BIIB021's mechanism of action as an orally available HSP90 inhibitor.
Main Results:
- BIIB021 exhibits potent antitumor activities across numerous preclinical cancer models.
- The compound is currently under clinical investigation for its therapeutic efficacy.
Conclusions:
- Targeting HSP90 with novel inhibitors like BIIB021 represents a promising strategy in cancer therapy.
- BIIB021's favorable profile warrants further clinical evaluation for its anti-cancer potential.
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