A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells

J Med Chem. 2024 Nov 28;67(22):20343-20352. doi: 10.1021/acs.jmedchem.4c01738. Epub 2024 Nov 15.

Abstract

Chronic dysregulation of microglial phenotypic balance contributes to prolonged neuroinflammation and neurotoxicity, which is a hallmark of neurodegenerative diseases. Thus, targeting microglial inflammatory signaling represents a promising therapeutic strategy for neurodegenerative diseases. Regulator of G protein Signaling 10 (RGS10) is highly expressed in microglia, where it suppresses pro-inflammatory signaling. However, RGS10 is silenced following microglial activation, augmenting inflammatory responses. While modulating RGS10 expression is a promising strategy to suppress pro-inflammatory microglial activation, no chemical tools with this ability exist. We developed a phenotypic high-throughput assay to screen for compounds with the ability to reverse interferon-γ (IFNγ)-induced RGS10 silencing in BV-2 cells. Identified hits had no effect on RGS10 expression in the absence of stimulus or in response to lipopolysaccharide (LPS). Furthermore, the hits reversed some of the inflammatory gene expression induced by IFNγ. This is the first demonstration of the potential for small molecule intervention to modulate the RGS10 expression in microglia.

MeSH terms

  • Animals
  • Cell Line
  • High-Throughput Screening Assays* / methods
  • Interferon-gamma* / metabolism
  • Interferon-gamma* / pharmacology
  • Lipopolysaccharides* / pharmacology
  • Mice
  • Microglia* / drug effects
  • Microglia* / metabolism
  • Phenotype
  • RGS Proteins* / genetics
  • RGS Proteins* / metabolism
  • Small Molecule Libraries* / chemistry
  • Small Molecule Libraries* / pharmacology

Substances

  • RGS Proteins
  • Interferon-gamma
  • Lipopolysaccharides
  • Small Molecule Libraries
  • Rgs10 protein, mouse