The quest for the shortest fragments of A (13-19) and B (12-17) responsible for the aggregation of human insulin

Nanomedicine (Lond). 2016 Aug;11(16):2083-101. doi: 10.2217/nnm-2016-0100. Epub 2016 Jul 27.

Abstract

Aim: To identify the shortest components of A13-A19, B12-B17 fragments capable for fibrillation and to validate the dependability of aggregation on the presence of hydroxyl group engaged in the 'tyrosine kissing'.

Materials & methods: Fragments A13-A19 and B12-B17 of insulin and all shortened analogues were obtained by using DMT/NMM/TosO(-) as a coupling reagent. The aggregation was studied by three independent tests.

Results: Studies on the susceptibility to aggregation of truncated analogs of insulin amyloidogenic core show three groups of peptides.

Conclusion: Truncation of A13-A419 fragment shows that fibrous structures are formed by all peptides bearing (13)H-LeuTyr-OH(14). Propensity to aggregation was found for (16)H-TyrLeu-OH(17) B12-B17 fragment. Tyrosine residue modification by incorporation of tert-butyl group on hydroxyl function gave analogues still predisposed to aggregation.

Keywords: aggregation; amyloid-like structure; diabetes; hydrophobic interaction; nanofibril; triazine coupling reagent; tyrosine residue; π–π interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Amyloid / chemistry*
  • Amyloid / metabolism
  • Amyloid / ultrastructure
  • Humans
  • Insulin / chemistry*
  • Insulin / metabolism
  • Leucine / chemistry
  • Leucine / metabolism
  • Peptide Fragments / chemistry*
  • Peptide Fragments / metabolism
  • Protein Aggregates*
  • Protein Aggregation, Pathological / metabolism
  • Tyrosine / chemistry
  • Tyrosine / metabolism

Substances

  • Amyloid
  • Insulin
  • Peptide Fragments
  • Protein Aggregates
  • Tyrosine
  • Leucine