d-Amino Acid Pseudopeptides as Potential Amyloid-Beta Aggregation Inhibitors

Molecules. 2018 Sep 18;23(9):2387. doi: 10.3390/molecules23092387.

Abstract

A causative factor for neurotoxicity associated with Alzheimer's disease is the aggregation of the amyloid-β (Aβ) peptide into soluble oligomers. Two all d-amino acid pseudo-peptides, SGB1 and SGD1, were designed to stop the aggregation. Molecular dynamics (MD) simulations have been carried out to study the interaction of the pseudo-peptides with both Aβ13⁻23 (the core recognition site of Aβ) and full-length Aβ1⁻42. Umbrella sampling MD calculations have been used to estimate the free energy of binding, ∆G, of these peptides to Aβ13⁻23. The highest ∆Gbinding is found for SGB1. Each of the pseudo-peptides was also docked to Aβ1⁻42 and subjected up to seven microseconds of all atom molecular dynamics simulations. The resulting structures lend insight into how the dynamics of Aβ1⁻42 are altered by complexation with the pseudo-peptides and confirmed that SGB1 may be a better candidate for developing into a drug to prevent Alzheimer's disease.

Keywords: Alzheimer’s; amyloid-beta; d-amino acids; inhibitors; molecular dynamics; umbrella sampling.

MeSH terms

  • Amino Acid Sequence
  • Amyloid beta-Peptides / chemistry
  • Amyloid beta-Peptides / metabolism*
  • Humans
  • Hydrogen Bonding
  • Molecular Docking Simulation
  • Molecular Dynamics Simulation
  • Monosaccharide Transport Proteins / chemistry
  • Monosaccharide Transport Proteins / metabolism
  • Nuclear Proteins / chemistry
  • Nuclear Proteins / metabolism
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Protein Aggregates / drug effects*
  • Protein Conformation
  • Protein Multimerization

Substances

  • Amyloid beta-Peptides
  • Monosaccharide Transport Proteins
  • Nuclear Proteins
  • Peptides
  • Protein Aggregates