Targeting of HDAC8 and investigational inhibitors in neuroblastoma

Expert Opin Investig Drugs. 2009 Nov;18(11):1605-17. doi: 10.1517/14728220903241658.

Abstract

Histone deacetylase (HDAC) inhibitors are an emerging class of promising novel anticancer drugs. However, little is known which one of the 11 classical HDAC family members is the most relevant drug target for therapy. The first Phase I/II trials show that unselective inhibition of HDACs causes a variety of side effects. Therefore, identification and selective targeting of the most critical tumor entity-relevant HDAC family member may reduce unspecific effects and increase antitumor efficacy in the future. Here, we review the clinical relevance of a particular HDAC family member, HDAC8, in neuroblastoma biology, a highly malignant embryonal childhood cancer. HDAC8 expression correlates with poor outcome in neuroblastoma and selective HDAC8 inhibition induces differentiation. In contrast, the targeting of other HDAC family members results in a completely different phenotype. Because HDAC8-selective inhibitors are available, HDAC8 may be a potential drug target for neuroblastoma differentiation therapy using selective inhibitors, avoiding unspecific side effects.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / pharmacology*
  • Child
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Drug Delivery Systems
  • Gene Expression Regulation, Neoplastic
  • Histone Deacetylases / genetics
  • Humans
  • Neuroblastoma / drug therapy*
  • Neuroblastoma / physiopathology
  • Repressor Proteins / antagonists & inhibitors*
  • Repressor Proteins / genetics

Substances

  • Antineoplastic Agents
  • Repressor Proteins
  • HDAC8 protein, human
  • Histone Deacetylases