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BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Aug 01; Vol. 20 (15), pp. 4639-44. Date of Electronic Publication: 2010 Jun 08. - Publication Year :
- 2010
-
Abstract
- Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transition state mimetic template. These inhibitors interact with the non prime side of the enzyme using a novel edge-to-face interaction with Arg-296.<br /> (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Alzheimer Disease drug therapy
Amyloid Precursor Protein Secretases chemistry
Amyloid Precursor Protein Secretases metabolism
Animals
Binding Sites
Computer Simulation
Crystallography, X-Ray
Ethylamines chemical synthesis
Ethylamines therapeutic use
Protease Inhibitors chemical synthesis
Protease Inhibitors therapeutic use
Rats
Structure-Activity Relationship
Amyloid Precursor Protein Secretases antagonists & inhibitors
Arginine chemistry
Ethylamines chemistry
Protease Inhibitors chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20579874
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.05.111