Metabolic resistance of Aβ3pE-42, a target epitope of the anti-Alzheimer therapeutic antibody, donanemab

Life Sci Alliance. 2024 Sep 30;7(12):e202402650. doi: 10.26508/lsa.202402650. Print 2024 Dec.

Abstract

The amyloid β peptide (Aβ), starting with pyroglutamate (pE) at position 3 and ending at position 42 (Aβ3pE-42), predominantly accumulates in the brains of Alzheimer's disease. Consistently, donanemab, a therapeutic antibody raised against Aβ3pE-42, has been shown to be effective in recent clinical trials. Although the primary Aβ produced physiologically is Aβ1-40/42, an explanation for how and why this physiological Aβ is converted to the pathological form remains elusive. Here, we present experimental evidence that accounts for the aging-associated Aβ3pE-42 deposition: Aβ3pE-42 was metabolically more stable than other Aβx-42 variants; deficiency of neprilysin, the major Aβ-degrading enzyme, induced a relatively selective deposition of Aβ3pE-42 in both APP transgenic and App knock-in mouse brains; Aβ3pE-42 deposition always colocalized with Pittsburgh compound B-positive cored plaques in APP transgenic mouse brains; and under aberrant conditions, such as a significant reduction in neprilysin activity, aminopeptidases, dipeptidyl peptidases, and glutaminyl-peptide cyclotransferase-like were up-regulated in the progression of aging, and a proportion of Aβ1-42 may be processed to Aβ3pE-42. Our findings suggest that anti-Aβ therapies are more effective if given before Aβ3pE-42 deposition.

MeSH terms

  • Alzheimer Disease* / drug therapy
  • Alzheimer Disease* / metabolism
  • Amyloid beta-Peptides* / metabolism
  • Amyloid beta-Protein Precursor / metabolism
  • Animals
  • Antibodies, Monoclonal, Humanized
  • Brain* / metabolism
  • Disease Models, Animal
  • Epitopes* / immunology
  • Epitopes* / metabolism
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic*
  • Neprilysin* / metabolism
  • Peptide Fragments / metabolism

Substances

  • Amyloid beta-Peptides
  • Neprilysin
  • Epitopes
  • Peptide Fragments
  • Amyloid beta-Protein Precursor
  • amyloid beta-protein (3-42), pyroglutamyl(3)-
  • donanemab
  • Antibodies, Monoclonal, Humanized