Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: A review

Eur J Med Chem. 2020 Apr 15:192:112171. doi: 10.1016/j.ejmech.2020.112171. Epub 2020 Feb 26.

Abstract

Among different Histone deacetylases (HDACs), histone deacetylase 3 (HDAC3) is an epigenetic drug target which is currently marked as a potential therapeutic strategy to combat various cancers. HDAC3 inhibitors are effective for the treatment of cancers, different neurodegenerative disorders, diabetes mellitus, cardiac diseases, HIV, inflammatory diseases, rheumatoid arthritis (RA), etc. Inhibition of HDAC3 metalloenzyme is a dynamic approach for drug design and discovery. This approach has gained considerable interest in recent years. The development of an effective therapeutic agent against HDAC3 is still challenging. A lot of work is still in demand. This current communication is a part of our extended work on HDAC3 inhibitors to achieve deep insight of knowledge about the structural information of HDAC3 inhibitors. This article is unique in terms of detailed structure-activity relationships (SARs) analysis. This may help to find out some important clues to design better active HDAC3 inhibitors in the future.

Keywords: Cancer; Drug design and discovery; HDAC3; HDAC3 inhibitor; Metalloenzyme; SAR.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histone Deacetylases / metabolism*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neurodegenerative Diseases / drug therapy
  • Neurodegenerative Diseases / metabolism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Histone Deacetylases
  • histone deacetylase 3