Natural and synthetic compounds as dissociated agonists of glucocorticoid receptor

Pharmacol Res. 2020 Jun:156:104802. doi: 10.1016/j.phrs.2020.104802. Epub 2020 Apr 8.

Abstract

Glucocorticoid receptor (GR) belongs to the superfamily of steroid hormone receptors. The dissociated or selective GR modulators (SEGRMs), preferring the transrepression rather than the transactivation, might exhibit anti-inflammatory activities with fewer side effects. This work presents a review of the molecular mechanism of GR involved in regulation of inflammation. As complementary or alternative therapeutic agents, the botanical compounds have been extensively used in the treatment of various diseases. Hence, this work reviews the botanical compounds as well as the synthetic compounds currently known to be potential SEGRMs. High-throughput virtual screening of SEGRMs from natural products has also been summarized.

Keywords: Dissociated characteristics; Natural products; Selective glucocorticoid receptor modulators; Transactivation; Transrepression.

Publication types

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

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / pharmacology*
  • Glucocorticoids / chemical synthesis
  • Glucocorticoids / pharmacology*
  • High-Throughput Screening Assays
  • Humans
  • Ligands
  • Molecular Structure
  • Phytochemicals / chemistry
  • Phytochemicals / pharmacology*
  • Receptors, Glucocorticoid / agonists*
  • Receptors, Glucocorticoid / metabolism
  • Signal Transduction
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Glucocorticoids
  • Ligands
  • Phytochemicals
  • Receptors, Glucocorticoid