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Structure-Based Discovery of Hsp90/HDAC6 Dual Inhibitors Targeting Aggressive Prostate Cancer.

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Related Experiment Video

Updated: Jun 14, 2025

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
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Searching for Novel HDAC6/Hsp90 Dual Inhibitors with Anti-Prostate Cancer Activity: In Silico Screening and In Vitro

Luca Pinzi1, Silvia Belluti1, Isabella Piccinini1

  • 1Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 103, 41125 Modena, Italy.

Pharmaceuticals (Basel, Switzerland)
|August 29, 2024
PubMed
Summary

Researchers screened compounds for dual inhibition of HDAC6 and Hsp90 to treat advanced prostate cancer (PCA). While compounds inhibited HDAC6 and reduced PCA cell growth, Hsp90 inhibition was not observed, suggesting optimization potential.

Keywords:
HDAC6Hsp90drug designprostate cancervirtual screening

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Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Prostate cancer (PCA) presents limited treatment options for advanced stages due to drug resistance.
  • Combined inhibition of histone deacetylase 6 (HDAC6) and heat shock protein 90 (Hsp90) offers potential synergistic effects against PCA.
  • HDAC6 and Hsp90 play crucial roles in regulating cancer cell processes.

Purpose of the Study:

  • To identify novel dual inhibitors targeting both HDAC6 and Hsp90 for advanced prostate cancer treatment.
  • To perform in silico virtual screening of commercial compounds for potential dual inhibitors.
  • To evaluate the in vitro efficacy of identified compounds against PCA cells.

Main Methods:

  • Extensive in silico virtual screening of commercial compound libraries.
  • In vitro enzyme inhibition assays against recombinant HDAC6.
  • Antiproliferative assays using LNCaP and PC-3 prostate cancer cell lines.

Main Results:

  • A subset of compounds demonstrated significant HDAC6 inhibitory activity.
  • Identified compounds exhibited antiproliferative effects on LNCaP and PC-3 cells.
  • No compounds showed significant Hsp90 inhibition, but possessed structural similarities to known Hsp90 inhibitors.

Conclusions:

  • The identified compounds are promising starting points for developing novel HDAC6/Hsp90 dual modulators.
  • Further medicinal chemistry optimization is warranted to enhance Hsp90 inhibitory activity.
  • These optimized compounds could offer improved therapeutic strategies for advanced prostate cancer.