Retinoid X Receptor as a Therapeutic Target to Treat Neurological Disorders Associated with α-Synucleinopathy

Cells. 2025 May 9;14(10):685. doi: 10.3390/cells14100685.

Abstract

This study investigated the therapeutic potential of the nuclear retinoid X receptor (RXR) in mitigating the progression of alpha-synucleinopathies (αSNPs), particularly in Parkinson's disease (PD). PD-like pathology in mice was successfully induced through the co-delivery of AAV expressing human α-synuclein (αS) and αS preformed fibrils (PFFs) into the substantia nigra pars compacta (SNpc). Significant increases in Lewy body (LB)-like inclusions, loss of tyrosine hydroxylase-positive (TH+) neurons, and reductions in dopamine (DA) levels in the striatum were observed. Additionally, diminished levels of PPARα and NURR1-proteins essential for neuronal survival-along with elevated expression of IBA1 and GFAP, markers of microglial activation and astrocytic gliosis, respectively, are associated with the pathogenesis of Parkinson's disease. AAV-mediated overexpression of human RXRα demonstrated preservation of TH+ neurons, prevention of DA decline, and attenuation of αS accumulation. Furthermore, RXR-treated PD brains showed a reduced number of GFAP+ and Iba1+ cells, decreased GFAP+ and IBA1+ immunoreactivity, and fewer and less widespread LB-like aggregates. RXR overexpression also enhanced the production of PPARα and NURR1. These findings suggest that RXRα upregulation promotes neuroprotection by mitigating αSNPs and chronic neuroinflammation, a major contributor to PD progression. This research underscores the therapeutic potential of targeting nuclear receptors, such as RXR, in neurodegenerative diseases like PD.

Keywords: Lewy body; NURR1; PPARα; Parkinson’s disease; dopamine; inflammation; retinoid X receptor; α-synuclein; α-synucleinopathy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Dopamine / metabolism
  • Dopaminergic Neurons / metabolism
  • Humans
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Microglia / metabolism
  • Neurons / metabolism
  • Neurons / pathology
  • Nuclear Receptor Subfamily 4, Group A, Member 2 / metabolism
  • PPAR alpha / metabolism
  • Parkinson Disease* / metabolism
  • Parkinson Disease* / pathology
  • Retinoid X Receptor alpha* / metabolism
  • Retinoid X Receptors* / metabolism
  • Synucleinopathies* / metabolism
  • Synucleinopathies* / pathology
  • Synucleinopathies* / therapy
  • Tyrosine 3-Monooxygenase / metabolism
  • alpha-Synuclein* / metabolism

Substances

  • alpha-Synuclein
  • Nuclear Receptor Subfamily 4, Group A, Member 2
  • Retinoid X Receptors
  • Dopamine
  • PPAR alpha
  • Retinoid X Receptor alpha
  • Tyrosine 3-Monooxygenase