Experimental approaches for elucidating co-agonist regulation of NMDA receptor in motor neurons: Therapeutic implications for amyotrophic lateral sclerosis (ALS)

J Pharm Biomed Anal. 2015 Dec 10:116:2-6. doi: 10.1016/j.jpba.2014.12.040. Epub 2015 Jan 3.

Abstract

Amyotrophic lateral sclerosis (ALS) is a neuromuscular disease characterised by selective loss of motor neurons leading to fatal paralysis. Although most cases are sporadic, approximately 10% of cases are familial and the identification of mutations in these kindred has greatly accelerated our understanding of disease mechanisms. To date, the causal genes in over 70% of these families have been identified. Recently, we reported a mutation (R199W) in the enzyme that degrades d-serine, D-amino acid oxidase (DAO) and co-segregates with disease in familial ALS. Moreover, D-serine and DAO are abundant in human spinal cord and severely depleted in ALS. Using cell culture models, we have defined the effects of R199W-DAO, and shown that it activates autophagy, leads to the formation of ubiquitinated protein aggregates and promotes apoptosis, all of which processes are attenuated by a D-serine/glycine site antagonist of the N-methyl D-aspartate receptor (NMDAR). These findings suggest that the toxic effects of R199W-DAO are at least in part mediated via the NMDAR involving the D-serine/glycine site and that an excitotoxic mechanism may contribute to disease pathogenesis.

Keywords: Amyotrophic lateral sclerosis (ALS); Glycine; Motor neurons; d-Amino acid oxidase (DAO); d-Serine.

Publication types

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

MeSH terms

  • Amyotrophic Lateral Sclerosis / drug therapy*
  • Amyotrophic Lateral Sclerosis / genetics
  • Amyotrophic Lateral Sclerosis / metabolism
  • Animals
  • D-Amino-Acid Oxidase / genetics
  • D-Amino-Acid Oxidase / metabolism
  • Excitatory Amino Acid Agonists / pharmacology
  • Excitatory Amino Acid Agonists / therapeutic use*
  • Humans
  • Motor Neurons / drug effects*
  • Motor Neurons / physiology
  • Receptors, N-Methyl-D-Aspartate / agonists*
  • Receptors, N-Methyl-D-Aspartate / physiology
  • Serine / genetics
  • Serine / metabolism

Substances

  • Excitatory Amino Acid Agonists
  • Receptors, N-Methyl-D-Aspartate
  • Serine
  • D-Amino-Acid Oxidase