AI Article Synopsis

  • Inhibition of BACE-1 could lead to new treatments for Alzheimer's disease.
  • The study involved creating potential drug candidates with the help of X-ray crystallography.
  • Discovered inhibitors effectively reduced amyloid production in laboratory tests.

Article Abstract

Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of potent inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic. These inhibitors were capable of lowering amyloid production in a cell-based assay.

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Source
http://dx.doi.org/10.1016/j.bmcl.2007.12.017DOI Listing

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