期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 6, 页码 1924-1927出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.139
关键词
Protease inhibitor; Peptidomimetic; Alzheimer's disease
资金
- NSERC of Canada
- Novartis (Basel, Switzerland)
Starting from peptidomimetic BACE-1 inhibitors, the P2 amino acid including the P2/P3 peptide bond was replaced by a rigid 3-aminomethyl cyclohexane carboxylic acid. Co-crystallization revealed an unexpected binding mode with the P3/P4 amide bond placed into the S3 pocket resulting in a new hydrogen bond interaction pattern. Further optimization based on this structure resulted in highly potent BACE-1 inhibitors with selectivity over BACE-2 and cathepsin D. (C) 2010 Elsevier Ltd. All rights reserved.
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