The Investigation on Resorcinarenes towards either Inhibiting or Promoting Insulin Fibrillation

Chemistry. 2017 Dec 19;23(71):17903-17907. doi: 10.1002/chem.201704932. Epub 2017 Dec 4.

Abstract

Different tail-engineered resorcinarenes have been examined for insulin fibrillation by experimental and computational studies. The resorcinarene showed a promising effect on the inhibition of insulin fibrillation, studied using a ThT assay, circular dichroism spectroscopy, and atomic force microscopy. Both the ThT assay and computational results indicate the tail from the resorcinarene has an impact on insulin fibrillation by either inhibition or promotion because of the resident position on insulin. These observations have significant biological implications in the design of drug molecules as well as the development of potential therapeutic strategies.

Keywords: biological chemistry; fibrillation; insulin; macrocycles; resorcinarene.

MeSH terms

  • Calixarenes / chemistry*
  • Calixarenes / metabolism
  • Circular Dichroism
  • Dynamic Light Scattering
  • Humans
  • Insulin / chemistry
  • Insulin / metabolism*
  • Kinetics
  • Microscopy, Atomic Force
  • Molecular Dynamics Simulation
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemistry
  • Phenylalanine / metabolism
  • Spectrometry, Fluorescence
  • Water / chemistry

Substances

  • Insulin
  • resorcinarene
  • Water
  • Calixarenes
  • Phenylalanine