The Amyloid Inhibitor CLR01 Relieves Autophagy and Ameliorates Neuropathology in a Severe Lysosomal Storage Disease

Mol Ther. 2020 Apr 8;28(4):1167-1176. doi: 10.1016/j.ymthe.2020.02.005. Epub 2020 Feb 12.

Abstract

Lysosomal storage diseases (LSDs) are inherited disorders caused by lysosomal deficiencies and characterized by dysfunction of the autophagy-lysosomal pathway (ALP) often associated with neurodegeneration. No cure is currently available to treat neuropathology in LSDs. By studying a mouse model of mucopolysaccharidosis (MPS) type IIIA, one of the most common and severe forms of LSDs, we found that multiple amyloid proteins including α-synuclein, prion protein (PrP), Tau, and amyloid β progressively aggregate in the brain. The amyloid deposits mostly build up in neuronal cell bodies concomitantly with neurodegeneration. Treating MPS-IIIA mice with CLR01, a "molecular tweezer" that acts as a broad-spectrum inhibitor of amyloid protein self-assembly reduced lysosomal enlargement and re-activates autophagy flux. Restoration of the ALP was associated with reduced neuroinflammation and amelioration of memory deficits. Together, these data provide evidence that brain deposition of amyloid proteins plays a gain of neurotoxic function in a severe LSD by affecting the ALP and identify CLR01 as new potent drug candidate for MPS-IIIA and likely for other LSDs.

Keywords: amyloid aggregation; autophagy; lysosomal storage disease; molecular tweezers; mucopolysaccharidosis type IIIA.

Publication types

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

MeSH terms

  • Amyloid / antagonists & inhibitors
  • Amyloid / metabolism
  • Animals
  • Autophagy / drug effects*
  • Brain / metabolism
  • Bridged-Ring Compounds / administration & dosage*
  • Bridged-Ring Compounds / pharmacology
  • Cell Body / metabolism
  • Disease Models, Animal
  • Male
  • Mice
  • Mucopolysaccharidosis III / complications
  • Mucopolysaccharidosis III / drug therapy*
  • Mucopolysaccharidosis III / metabolism
  • Neurodegenerative Diseases / drug therapy*
  • Neurodegenerative Diseases / etiology
  • Organophosphates / administration & dosage*
  • Organophosphates / pharmacology
  • Treatment Outcome

Substances

  • Amyloid
  • Bridged-Ring Compounds
  • CLR01 compound
  • Organophosphates