Histone deacetylase inhibitors: a chemical genetics approach to understanding cellular functions

Biochim Biophys Acta. 2010 Oct-Dec;1799(10-12):717-25. doi: 10.1016/j.bbagrm.2010.05.008. Epub 2010 Jun 8.

Abstract

There are eleven zinc dependent histone deacetylases (HDAC) in humans which have histones and many non-histone substrates. The substrates of these enzymes include proteins that have a role in regulation of gene expression, cell proliferation, cell migration, cell death, immune pathways and angiogenesis. Inhibitors of HDACs (HDACi) have been developed which alter the structure and function of these proteins, causing molecular and cellular changes that induce transformed cell death. The HDACi are being developed as anti-cancer drugs and have therapeutic potential for many non-oncologic diseases.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use
  • Cell Death / drug effects
  • Cell Movement / drug effects
  • Cell Movement / genetics
  • Cell Proliferation / drug effects
  • Gene Expression Regulation / drug effects
  • Gene Expression Regulation / genetics
  • Histone Deacetylase Inhibitors / chemistry*
  • Histone Deacetylase Inhibitors / metabolism*
  • Histone Deacetylase Inhibitors / therapeutic use
  • Histone Deacetylases / chemistry*
  • Histone Deacetylases / genetics*
  • Histone Deacetylases / metabolism*
  • Humans
  • Neovascularization, Physiologic / drug effects
  • Neovascularization, Physiologic / genetics
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Histone Deacetylases