Panobinostat: The Small Molecule Metalloenzyme Inhibitor with Marvelous Anticancer Activity

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Assays for Validating Histone Acetyltransferase Inhibitors
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Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

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Shabir Ahmad Ganai1

  • 1Centre for Nanotechnology & Advanced Biomaterials (CeNTAB), School of Chemical & Biotechnology, SASTRA University, Thanjavur, Tamil Nadu, India. Shabir.muntazir82@gmail.com.

Current Topics in Medicinal Chemistry
|August 14, 2015
PubMed

Insights

Panobinostat, a histone deacetylase inhibitor (HDACi), shows antiproliferative effects against various cancers. Combination strategies may enhance its therapeutic benefits and overcome resistance.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Histone acetyl transferases (HATs) and histone deacetylases (HDACs) regulate gene expression through histone acetylation.
  • Deregulation of HDACs is implicated in cancer development and progression, making them therapeutic targets.
  • Histone deacetylase inhibitors (HDACi) demonstrate anticancer effects like cell cycle arrest and apoptosis.

Purpose of the Study:

  • To review the antiproliferative activity of panobinostat, a pan-HDAC inhibitor.
  • To detail the mechanisms of panobinostat's cytotoxic effects in various cancers.
  • To explore combination strategies for panobinostat to enhance therapeutic outcomes and overcome resistance.

Main Methods:

  • Review of literature on panobinostat (LBH589).
  • Analysis of antiproliferative activity in breast, ovarian, lung cancers, and multiple myeloma.
  • Examination of cytotoxic mechanisms and combination therapies.

Main Results:

  • Panobinostat exhibits antiproliferative activity across multiple cancer types.
  • Detailed mechanisms of panobinostat-induced cytotoxicity are elucidated.
  • Combination strategies show potential for overcoming therapy resistance.

Conclusions:

  • Panobinostat is a promising pan-HDAC inhibitor with broad-spectrum anticancer activity.
  • Understanding its mechanisms and combination potential is crucial for future cancer therapy.
  • Panobinostat offers a valuable therapeutic option, especially in resistant cancer cases.

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