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Spotlight on 17-AAG as an Hsp90 inhibitor for molecular targeted cancer treatment

Sona Talaei1,2, Hassan Mellatyar1,2, Asadollah Asadi3

  • 1Hematology and Oncology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

Chemical Biology & Drug Design
|January 31, 2019
PubMed

Insights

Heat shock protein 90 (Hsp90) is a cancer therapeutic target. 17-allylamino-17-demethoxy-geldanamycin (17-AAG) inhibits Hsp90, but faces challenges. Nanomaterials may improve its cancer treatment efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Delivery

Background:

  • Heat shock protein 90 (Hsp90) is crucial for cancer cell survival and progression.
  • Hsp90 client proteins are involved in multiple oncogenic pathways, making Hsp90 a viable cancer therapeutic target.
  • 17-allylamino-17-demethoxy-geldanamycin (17-AAG) is a potent Hsp90 inhibitor that induces client protein degradation.

Purpose of the Study:

  • To review preclinical and clinical research on 17-AAG as a single agent and in combination therapies.
  • To highlight the potential of nanocarriers and nanocombination therapy to overcome 17-AAG's limitations.
  • To explore strategies for improving the therapeutic efficacy of Hsp90 inhibition in cancer treatment.

Main Methods:

  • Review of preclinical studies evaluating 17-AAG efficacy and safety.
  • Analysis of clinical trial data for 17-AAG in various human cancers.
  • Exploration of nanocarrier-based drug delivery systems for 17-AAG.

Main Results:

  • 17-AAG demonstrates biological activity and safety at therapeutic doses, with mild toxicity.
  • Preclinical studies show promise for 17-AAG as a single agent and in combination therapies.
  • Low water solubility and high hepatotoxicity of 17-AAG limit its clinical application.

Conclusions:

  • Nanomaterials-based drug delivery offers a promising strategy to overcome 17-AAG's limitations.
  • Nanocarrier-mediated delivery and nanocombination therapy can enhance the therapeutic effects of 17-AAG.
  • Further research into nanocarrier applications is warranted to optimize 17-AAG-based cancer treatments.
Keywords:
17-AAGHsp90Hsp90 client proteinscancer therapy

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