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Cited by 311Heat shock proteins researchProtein Degradation and InhibitorsHistone Deacetylase Inhibitors Research

Update on Hsp90 Inhibitors in Clinical Trial

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Kim, Y., Alarcon, S., Lee, S., Lee, M.-J., Giaccone, G., Neckers, L., Trepel, J.·2009·Current Topics in Medicinal Chemistry
DOI 10.2174/156802609789895728PMC PMC7241864
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Abstract

Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinical trials in 1999. There are now 13 Hsp90 inhibitors in clinical trial, representing multiple drug classes, and hundreds of patients have been treated in adult oncology and pediatric oncology trials. This review will provide an overview of the clinical trial results thus far. In addition, pivotal issues in further development of Hsp90 inhibitors as anticancer drugs will be discussed.

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References 48 · Cited by 311

Research works printed but not linked: 38

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Authors
Kim, Y., Alarcon, S., Lee, S., Lee, M.-J., Giaccone, G., Neckers, L., & Trepel, J.
Affiliations
National Institutes of Health (US)
Corresponding author
Trepel, J.
ORCID
Venue
Current Topics in Medicinal Chemistry
Publisher
Bentham Science Publishers Ltd.
Published
2009-11-01
Volume
9
Issue
15
Pages
1479-1492
ISSN
1568-0266 (ISSN-L)
DOI
10.2174/156802609789895728
PMC
PMC7241864
OpenAlex
W2116393881
Cited by
311
References
48
Citations by year
2026: 4 · 2025: 9 · 2024: 22 · 2023: 11 · 2022: 12 · 2021: 16 · 2020: 9 · 2019: 11 · 2018: 9 · 2017: 11 · 2016: 13 · 2015: 20 · 2014: 18 · 2013: 31 · 2012: 51
FWCI
15.95
Type
journal article
Language
en
Open access
Locations
  • Current Topics in Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
Funders
  • National Institutes of Health
  • National Cancer Institute (Z01SC010074, Z01BC010854)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Heat shock proteins research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
Keywords
Hsp90 inhibitors, Hsp90 chaperone, 17-AAG, anticancer agents, clinical trials, pediatric oncology, adult oncology, small molecule inhibitors, drug development
MeSH terms
Antineoplastic Agents, Clinical Trials as Topic, Humans, Neoplasms, HSP90 Heat-Shock Proteins

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