Logo image
Designed Amyloid β Peptide Fibril—A Tool for High‐Throughput Screening of Fibril Inhibitors
Article de revue scientifique   Avec comité de lecture

Designed Amyloid β Peptide Fibril—A Tool for High‐Throughput Screening of Fibril Inhibitors

Gunnar Dolphin, Myriam Ouberai, Pascal Dumy et Julian Garcia
ChemMedChem, Vol.2(11), p.1613-1623
12/11/2007
PMID: 17876751

Résumé

Amyloid beta-Peptides Chemical Sciences Drug Design Life Sciences Pharmaceutical sciences Pharmacology Protein Folding Reproducibility of Results
Amyloid β peptide (Aβ) fibril formation is widely believed to be the causative event of Alzheimer’s disease pathogenesis. Therapeutic approaches are therefore in development that target various sites in the production and aggregation of Aβ. Herein we present a high-throughput screening tool to generate novel hit compounds that block Aβ fibril formation. This tool is an application for our fibril model (Aβ16–37Y20K22K24)4, which is a covalent assembly of four Aβ fragments. With this tool, screening studies are complete within one hour, as opposed to days with native Aβ1–40. A Z′ factor of 0.84±0.03 was determined for fibril formation and inhibition, followed by the reporter molecule thioflavin T. Herein we also describe the analysis of a broad range of reported inhibitors and non-inhibitors of Aβ fibril formation to test the validity of the system.

Indicateurs

1 Consultations de la notice

Détails

Logo image