The DOI matches its Crossref record.
HSP90 Inhibitors: Current Development and Potential in Cancer Therapy
Abstract
In the last decade, the molecular chaperone HSP90 has emerged as an important target in cancer therapeutics and has subsequently become the focus of several drug discovery and development efforts. The first-in-class HSP90 inhibitor 17-AAG entered into Phase I clinical trial in 1999. Today 13 HSP90 inhibitors representing multiple drug classes, with different modes of action, are undergoing clinical evaluation. The present review will highlight the involvement of HSP90 in regulating and maintaining the transformed phenotype, provide an overview on current HSP90 inhibitors and further update on the most relevant patents which have recently appeared in the literature. Keywords: Cancer therapeutics, cell surface, chaperoning, drug discovery, HSP90, signal transduction.
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In the citing paper
“However, to date, there are no clinically approved HSP90 inhibitors, as most trials have been associated with limited efficacy and significant toxicity”
From Bruton tyrosine kinase degradation as a therapeutic strategy for cancer (2019) · cites this paper as [11]
In the citing paper
“presumably because HSP90 inhibition promotes the degradation of different substrates in different tissues and rapidly induces stress responses that may mediate resistance.11”
From Bruton tyrosine kinase degradation as a therapeutic strategy for cancer (2019) · cites this paper as [11]
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Heat shock proteins: Biological functions, pathological roles, and therapeutic opportunities
Hu, C., Yang, J. C., Qi, Z., Wu, H., Wang, B., Zou, F., Mei, H., Liu, J. L., Wang, W., & Liu, Q. (2022) · MedComm · doi:10.1002/mco2.161 · Cited by 881
Heat Shock Proteins and Cancer
Wu, J., Liu, T., Rios, Z., Mei, Q., Lin, X., & Cao, S. (2016) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2016.11.009 · Cited by 726
The HSP90 Family: Structure, Regulation, Function, and Implications in Health and Disease
Hoter, A., El-Sabban, M. E., & Naim, H. Y. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19092560 · Cited by 693
“Natural products like geldanamycin (GA) that was derived from Streptomyces hygroscopicus and the antibiotic radicicol (RD), isolated from Monosporium bonorden exhibited prominent suppression of tumor proliferation and growth [189,190].”
BackgroundChaperone-mediated autophagy is involved in the execution of ferroptosis
Wu, Z., Geng, Y., Lu, X., Shi, Y., Wu, G., Zhang, M., Shan, B., Pan, H., & Yuan, J. (2019) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1819728116 · Cited by 582
“Heat shock protein 90 (HSP90), an evolutionary conserved and ubiquitously expressed molecular chaperone, plays an important role in maintaining the function and stability of cellular proteins (21, 22).”
BackgroundGoh, G., Walradt, T. J., Markarov, V., Blom, A., Riaz, N., Doumani, R., Stafstrom, K., Moshiri, A. S., Yelistratova, L., Levinsohn, J. L., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.6494 · Cited by 396
“The pan-HDAC inhibitor, SAHA, is FDA-approved, and HSP90 inhibitors [30] are currently in clinical trials.”
Background
Metadata
- Authors
- Sidera, K., & Patsavoudi, E.
- Affiliations
- Pasteur Hellenic Institute (GR)
- Venue
- Recent Patents on Anti-Cancer Drug Discovery
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2013-12-13
- Volume
- 9
- Issue
- 1
- Pages
- 1-20
- ISSN
- 1574-8928 (ISSN-L)
- OpenAlex
- W4245469960
- Cited by
- 222
- References
- 0
- Citations by year
- 2026: 3 · 2025: 7 · 2024: 8 · 2023: 17 · 2022: 14 · 2021: 28 · 2020: 21 · 2019: 31 · 2018: 18 · 2017: 19 · 2016: 28 · 2015: 19 · 2014: 8 · 2013: 1
- FWCI
- 8.35
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Recent Patents on Anti-Cancer Drug Discovery (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Heat shock proteins research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
- Keywords
- Hsp90 inhibitors, HSP90, molecular chaperones, cancer therapeutics, 17-AAG, drug discovery, clinical trials, patents, transformed phenotype, signal transduction, cell surface
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