Inhibitors selective for HDAC6 in enzymes and cells

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. doi: 10.1016/j.bmcl.2010.09.100. Epub 2010 Oct 12.

Abstract

Histone deacetylase inhibitors with anticancer or anti-inflammatory activity bind to Class I or Class I and II HDAC enzymes. Here we compare selectivity of inhibitors of a Class II HDAC enzyme (HDAC6) and find one that retains high selectivity in macrophages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry*
  • Antineoplastic Agents / chemistry*
  • Cell Line
  • Histone Deacetylase 1 / drug effects
  • Histone Deacetylase 6
  • Histone Deacetylase Inhibitors / chemistry*
  • Histone Deacetylases / drug effects
  • Humans
  • Macrophages / enzymology
  • Mice
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • HDAC1 protein, human
  • HDAC6 protein, human
  • Histone Deacetylase 1
  • Histone Deacetylase 6
  • Histone Deacetylases