HSP90 and Its Inhibitors for Cancer Therapy: Use of Nano-delivery System to Improve Its Clinical Application

  • Prathap Somu
  • Subhankar PaulEmail author
Part of the Heat Shock Proteins book series (HESP, volume 19)


The molecular chaperone HSP90 (heat shock protein 90) has become a crucial target in cancer therapeutics as its function has been implicated with various types of malignant transformation. Numerous HSP90 inhibitors have been identified so far and many of them have also been clinically tested. Although most of these are natural or their derived inhibitors including geldanamycin and its derivatives 17-AAG and 17-DMAG have shown efficacy, their easy success has been hindered in various stages of the clinical studies due to poor solubility and cytotoxicity. However, recently substantial published documents reported that the systemic targeting of the HSP90 inhibitors using nano-based drug delivery system could provide a possible clinical solution to overcome their limitation. In this chapter, we review the initial development of various HSP90 inhibitors from natural to synthetically derived one and their clinical studies. We also review their limitations and future perspectives as a possible potential agent in the cancer therapeutics by their systemic and control delivery to the target site using the nano-drug delivery system. Also, the application of combined therapy has also been discussed in the current chapter using HSP90 inhibitors and nanocarrier. In addition, we also discuss the therapeutic approaches like photothermal where nano carrier is not only used as a carrier for the systemic delivery of HSP90 inhibitors but also as a therapeutic agent.


Cancer Heat shock proteins Molecular chaperone Nanomaterials Targeted delivery Therapeutic index 







adenosine diphosphate


aryl hydrocarbon receptor


adenosine triphosphate


clinical benefit rate


dose-limiting toxicities


Epigallocatechin 3-gallate


fluorodeoxyglucose positron emission tomography


gastrointestinal stromal tumors




HSP90 organizing protein


heat shock protein


17-desmethoxy-17-amino Geldanamycin


17-allylamino-17-demethoxygeldanamycin Hydroquinone Hydro-chloride


multi-drug resistance


maximum tolerated dose


non-small-cell lung carcinoma


overall response rate


peripheral blood mononuclear cells




platelet-derived growth factor receptor alpha


poly(ethylene glycol)


positron emission tomography


poly (lactic-co-glycolic acid)


partial response




stable diseases


standardized uptake value


triple-negative breast cancer



The authors sincerely thank the Science and Engineering Research Board, Government of India, for financial support (Grant No. SERB/F/4290/2016-17) and National Institute of Technology Rourkela, Government of India, for providing the infrastructural facility for the preparation of the chapter.


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Authors and Affiliations

  1. 1.Structural Biology & Nanomedicine Laboratory, Department of Biotechnology & Medical EngineeringNational Institute of Technology RourkelaRourkelaIndia

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