title: Effect of chirality of small molecule organofluorine inhibitors of amyloid self-assembly on inhibitor potency.
abstract: The effect of enantiomeric trifluoromethyl-indolyl-acetic acid ethyl esters on the fibrillogenesis of Alzheimer's amyloid beta (Abeta) peptide is described. These compounds have been previously identified as effective inhibitors of the Abeta 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 Abeta peptide.
authors.affiliation: Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd. Boston, MA 02125-3393, USA.
authors.forename: Abha
authors.initials: A
authors.lastname: Sood
authors.forename: Mohammed
authors.initials: M
authors.lastname: Abid
authors.forename: Samson
authors.initials: S
authors.lastname: Hailemichael
authors.forename: Michelle
authors.initials: M
authors.lastname: Foster
authors.forename: Béla
authors.initials: B
authors.lastname: Török
authors.forename: Marianna
authors.initials: M
authors.lastname: Török
mesh_terms: D000544:Alzheimer Disease / Q000378:metabolism*; D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005461:Fluorine / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D018625:Microscopy, Atomic Force; D011422:Propionates / Q000737:chemistry / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013237:Stereoisomerism
chemical_list: D016229:Amyloid beta-Peptides; D011422:Propionates; D005461:Fluorine