Effect of chirality of small molecule organofluorine inhibitors of amyloid self-assembly on inhibitor potency

  • Abha Sood
  • , Abid Shaikh
  • , Samson Hailemichael
  • , Michelle Foster
  • , Béla Török
  • , Marianna Török

Research output: Contribution to journalArticlepeer-review

32 Scopus citations
3 Downloads (Pure)

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.

Original languageEnglish
Pages (from-to)6931-6934
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number24
DOIs
StatePublished - Dec 15 2009

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Keywords

  • Amyloid-beta peptide
  • Chiral
  • Fibrillogenesis
  • Organofluorine
  • Small molecule inhibitor

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