Nuclear receptor coregulators as a new paradigm for therapeutic targeting

Elaine Y. Hsia, Michael L. Goodson, June X Zou, Martin L. Privalsky, Hongwu Chen

Research output: Contribution to journalArticlepeer-review

46 Scopus citations


The complex function and regulation of nuclear receptors cannot be fully understood without a thorough knowledge of the receptor-associated coregulators that either enhance (coactivators) or inhibit (corepressors) transcription. While nuclear receptors themselves have garnered much attention as therapeutic targets, the clinical and etiological relevance of the coregulators to human diseases is increasingly recognized. Aberrant expression or function of coactivators and corepressors has been associated with malignant and metabolic disease development. Many of them are key epigenetic regulators and utilize enzymatic activities to modify chromatin through histone acetylation/deacetylation, histone methylation/demethylation or chromatin remodeling. In this review, we showcase and evaluate coregulators - such as SRCs and ANCCA - with the most promising therapeutic potential based on their physiological roles and involvement in various diseases that are revealed thus far. We also describe the structural features of the coactivator and corepressor functional domains and highlight areas that can be further explored for molecular targeting.

Original languageEnglish (US)
Pages (from-to)1227-1237
Number of pages11
JournalAdvanced Drug Delivery Reviews
Issue number13
StatePublished - Oct 30 2010


  • Cancer
  • Diabetes
  • Histone acetylation
  • Histone methylation
  • NCoR
  • Obesity
  • P160/SRC
  • PGC-1
  • SMRT

ASJC Scopus subject areas

  • Pharmaceutical Science


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