APOE Genotype Difference in the Biphasic Modulation of Amyloid-β Aggregation by Direct Binding and Lowering the Nucleation Barrier

Biomacromolecules. 2025 Dec 8;26(12):8494-8507. doi: 10.1021/acs.biomac.5c01323. Epub 2025 Nov 3.

Abstract

Amyloid-β (Aβ) aggregation is a hallmark of Alzheimer's disease (AD), while the apoE4 isoform (C112R) represents the strongest genetic risk factor. We combined binding-site mapping and discrete molecular dynamics (DMD) simulations to elucidate isoform-specific apoE-Aβ interactions. Computational peptide-array analysis identified Aβ-binding hotspots in the apoE4 N-terminal domain (NTD) around R112, conferring greater Aβ-binding propensity than apoE3. DMD simulations showed that apoE4 NTD is less stable and more solvent-exposed, resulting in stronger Aβ binding, especially near the mutation site. Upon binding apoE NTDs, Aβ exhibited an increased β-sheet content, suggesting a lowered fibril nucleation barrier. Incorporating these insights into a recently established thermodynamic-kinetic framework of amyloid aggregation rationalizes apoE's biphasic effect on Aβ aggregation: apoE retards Aβ fibrillization at low Aβ-concentrations via monomer sequestration but accelerates the process at high concentrations by facilitating nucleation. Our findings offer mechanistic insight into the APOE genotype-dependent modulation of Aβ aggregation and may inform genotype-specific therapeutic strategies for AD.

MeSH terms

  • Alzheimer Disease / genetics
  • Alzheimer Disease / metabolism
  • Amyloid beta-Peptides* / chemistry
  • Amyloid beta-Peptides* / genetics
  • Amyloid beta-Peptides* / metabolism
  • Apolipoprotein E3* / chemistry
  • Apolipoprotein E3* / genetics
  • Apolipoprotein E3* / metabolism
  • Apolipoprotein E4* / chemistry
  • Apolipoprotein E4* / genetics
  • Apolipoprotein E4* / metabolism
  • Apolipoproteins E* / chemistry
  • Apolipoproteins E* / genetics
  • Apolipoproteins E* / metabolism
  • Binding Sites
  • Genotype
  • Humans
  • Molecular Dynamics Simulation
  • Protein Aggregates
  • Protein Binding

Substances

  • Amyloid beta-Peptides
  • Apolipoprotein E4
  • Apolipoproteins E
  • Protein Aggregates
  • Apolipoprotein E3