Anti-α-synuclein ASO delivered to monoamine neurons prevents α-synuclein accumulation in a Parkinson's disease-like mouse model and in monkeys

EBioMedicine. 2020 Sep:59:102944. doi: 10.1016/j.ebiom.2020.102944. Epub 2020 Aug 15.

Abstract

Background: Progressive neuronal death in monoaminergic nuclei and widespread accumulation of α-synuclein are neuropathological hallmarks of Parkinson's disease (PD). Given that α-synuclein may be an early mediator of the pathological cascade that ultimately leads to neurodegeneration, decreased α-synuclein synthesis will abate neurotoxicity if delivered to the key affected neurons.

Methods: We used a non-viral gene therapy based on a new indatraline-conjugated antisense oligonucleotide (IND-ASO) to disrupt the α-synuclein mRNA transcription selectively in monoamine neurons of a PD-like mouse model and elderly nonhuman primates. Molecular, cell biology, histological, neurochemical and behavioral assays were performed.

Findings: Intracerebroventricular and intranasal IND-ASO administration for four weeks in a mouse model with AAV-mediated wild-type human α-synuclein overexpression in dopamine neurons prevented the synthesis and accumulation of α-synuclein in the connected brain regions, improving dopamine neurotransmission. Likewise, the four-week IND-ASO treatment led to decreased levels of endogenous α-synuclein protein in the midbrain monoamine nuclei of nonhuman primates, which are affected early in PD.

Conclusions: The inhibition of α-synuclein production in dopamine neurons and its accumulation in cortical/striatal projection areas may alleviate the early deficits of dopamine function, showing the high translational value of antisense oligonucleotides as a disease modifying therapy for PD and related synucleinopathies.

Funding: Grants SAF2016-75797-R, RTC-2014-2812-1 and RTC-2015-3309-1, Ministry of Economy and Competitiveness (MINECO) and European Regional Development Fund (ERDF), UE; Grant ID 9238, Michael J. Fox Foundation; and Centres for Networked Biomedical Research on Mental Health (CIBERSAM), and on Neurodegenerative Diseases (CIBERNED).

Keywords: Antisense oligonucleotide; Axonal neurodegeneration; Dopamine neurotransmission; Mouse and monkey models; Parkinson's disease; α-Synuclein.

MeSH terms

  • Animals
  • Behavior, Animal
  • Disease Models, Animal
  • Female
  • Gene Expression
  • Gene Transfer Techniques
  • Genetic Therapy
  • Genetic Vectors / genetics
  • Haplorhini
  • Humans
  • Immunohistochemistry
  • Male
  • Mice
  • Morris Water Maze Test
  • Neurons / metabolism*
  • Oligonucleotides, Antisense / administration & dosage*
  • Parkinson Disease / diagnosis
  • Parkinson Disease / etiology
  • Parkinson Disease / metabolism*
  • Parkinson Disease / therapy
  • Synaptic Transmission
  • Treatment Outcome
  • alpha-Synuclein / genetics*
  • alpha-Synuclein / metabolism*

Substances

  • Oligonucleotides, Antisense
  • SNCA protein, human
  • alpha-Synuclein