Skip to main content
Article
Effect of Chirality of Small Molecule Organofluorine Inhibitors of Amyloid Self-Assembly on Inhibitor Potency
Bioorganic and Medicinal Chemistry Letters (2009)
  • Abha Sood, University of Massachusetts
  • Abid Shaikh, Georgia Southern University
  • Samson Hailemichael, University of Massachusetts
  • Michelle Foster, University of Massachusetts
  • Béla Török
  • Marianna Török
Abstract
The effect of enantiomeric trifluoromethyl-indolyl-acetic acid ethyl esters on the fibrillogenesis of Alzheimer’s amyloid β (Aβ) peptide is described. These compounds have been previously identified as effective inhibitors of the Aβ self-assembly in their racemic form. Thioflavin-T Fluorescence Spectroscopy and Atomic Force Microscopy were applied to assess the potency of the chiral target compounds. Both enantiomers showed significant inhibition in the in vitro assays. The potency of the enantiomeric inhibitors appeared to be very similar to each other suggesting the lack of the stereospecific binding interactions between these small molecule inhibitors and the Aβ peptide.
Keywords
  • Amyloid-beta peptide,
  • Fibrillogenesis,
  • Small molecule inhibitor,
  • Chiral,
  • Organofluorine
Disciplines
Publication Date
2009
Publisher Statement
This is an Accepted Author Manuscript obtained from PMC. The publisher's final edited version of this article is available at Bioorganic and Medicinal Chemistry Letters.
Citation Information
Abha Sood, Abid Shaikh, Samson Hailemichael, Michelle Foster, Béla Török, and Marianna Török. "Effect of Chirality of Small Molecule Organofluorine Inhibitors of Amyloid Self-Assembly on Inhibitor Potency" Bioorganic and Medicinal Chemistry Letters 19.24 (2009): 6931-6934.
doi:10.1016/j.bmcl.2009.10.066
source:http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2785120/
Available at: http://works.bepress.com/abid_shaikh/5