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Targeting Hsp90: small-molecule inhibitors and their clinical development
Open accessAbstract
The Hsp90 multichaperone complex has important roles in the development and progression of malignant transformation. Several small-molecule inhibitors of Hsp90 of diverse chemotypes have shown potent antitumor activity in a wide-range of malignancies, and are currently in clinical or late-stage preclinical investigation. This review intends to update the reader on advances made over the past two years in the clinical development of Hsp90 inhibitors in advanced cancers. It will refer to the two 17-AAG formulations, tanespimycin and IPI-504, and to synthetic small molecules, among which are the purine-scaffold Hsp90 inhibitor CNF2024/BIIB021, the isoxazole derivative VER-52296/NVP-AUY922, and the carbazol-4-one benzamide derivative SNX-5422, and will present our current knowledge on their clinical performance.
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Citations
Cites
HSP90 and the chaperoning of cancer
Whitesell, L., & Lindquist, S. L. (2005) · Nature Reviews Cancer · doi:10.1038/nrc1716 · Cited by 2,502
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Biological and Chemical Approaches to Diseases of Proteostasis Deficiency
Powers, E. T., Morimoto, R. I., Dillin, A., Kelly, J. W., & Balch, W. E. (2009) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.052308.114844 · Cited by 1,149
Protein Folding in the Cytoplasm and the Heat Shock Response
Vabulas, R. M., Raychaudhuri, S., Hayer-Hartl, M., & Hartl, F. U. (2010) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a004390 · Cited by 428
Cowen, L. E., Singh, S. D., Köhler, J. R., Collins, C., Zaas, A. K., Schell, W. A., Aziz, H., Mylonakis, E., Perfect, J. R., Whitesell, L., et al. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0813394106 · Cited by 413
Jackson, S. E. (2012) · Topics in Current Chemistry · doi:10.1007/128_2012_356 · Cited by 338
Metadata
- Authors
- Taldone, T., Gozman, A., Maharaj, R., & Chiosis, G.
- Venue
- Current Opinion in Pharmacology
- Publisher
- Elsevier BV
- Published
- 2008-08
- Volume
- 8
- Issue
- 4
- Pages
- 370-374
- ISSN
- 1471-4892 (ISSN-L)
- OpenAlex
- W1970700441
- Cited by
- 284
- References
- 1
- FWCI
- 14.64
- Type
- journal article
- Language
- en
- Open access
- green
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- Taldone, T., Gozman, A., Maharaj, R., & Chiosis, G. (2008). Targeting Hsp90: small-molecule inhibitors and their clinical development. Current Opinion in Pharmacology. https://doi.org/10.1016/j.coph.2008.06.015
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
