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Updated: May 21, 2025

Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
Recent progress and structural insights of potential Hsp90 inhibitors as anticancer agents
Aastha Singh1, Subhadip Maity1, Priya Devi1
1Department of Pharmaceutical Analysis, ISF College of Pharmacy, Moga, Punjab, India.
Abstract:
Hsp90, or heat shock protein 90, a well-preserved molecular chaperone that is essential for the coordination of numerous biological pathways and cellular processes. Hsp90 is a molecular chaperone, which promises a target for cancer treatment. Hsp90 inhibitors are a class of drugs that have been extensively studied in preclinical models and demonstrated promise in treating a variety of illnesses, particularly cancer. Hsp90 inhibitors, however, have been encountered a number of challenges during the clinical development process, such as low efficacy, toxicity, and drug resistance. This literature survey emphasizes the importance of HSP90 inhibitors incorporating diverse heterocyclic rings, such as pyrazole, indole, pyrimidine, triazole, and thioquinazoline, which have exhibited promising anticancer activity. This review covers several parameters, including kinetic investigation, binding interactions, IC50 value, structure-activity relationship, and molecular docking studies of the most potent compound. There are several heterocyclic small molecules under investigation in clinical studies, such as AUY922, SNX-5422, STA-9090, and others. This review also contained a patent of HSP90 inhibitors, which showed greater effectiveness. Therefore, the main objective of this paper is to summarize all recent developments in the creation of anticancer medications that target HSP90 inhibitors in order to treat anticancer disease.
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