Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.

Machauer, Rainer; Veenstra, Siem; Rondeau, Jean-Michel; Tintelnot-Blomley, Marina; Betschart, Claudia; Neumann, Ulf; Paganetti, Paolo

Machauer, Rainer; Veenstra, Siem; Rondeau, Jean-Michel; Tintelnot-Blomley, Marina; Betschart, Claudia; Neumann, Ulf; Paganetti, Paolo.

Affiliation

Machauer R; Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH-4002 Basel, Switzerland.

Bioorg Med Chem Lett ; 19(5): 1361-5, 2009 Mar 01.

Article in En | MEDLINE | ID: mdl-19195886

Subject(s)

Amyloid Precursor Protein Secretases/antagonists & inhibitors; Aspartic Acid Endopeptidases/antagonists & inhibitors; Protease Inhibitors/chemical synthesis; Amyloid Precursor Protein Secretases/chemistry; Amyloid Precursor Protein Secretases/metabolism; Animals; Aspartic Acid Endopeptidases/chemistry; Aspartic Acid Endopeptidases/metabolism; Binding Sites/physiology; Biomimetic Materials/chemistry; Biomimetic Materials/pharmacology; CHO Cells; Cricetinae; Cricetulus; Crystallography, X-Ray; Humans; Macrocyclic Compounds/chemistry; Macrocyclic Compounds/pharmacology; Oligopeptides/chemical synthesis; Oligopeptides/pharmacology; Peptide Fragments/chemical synthesis; Peptide Fragments/pharmacology; Protease Inhibitors/pharmacology; Protein Structure, Tertiary/physiology; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protease Inhibitors / Aspartic Acid Endopeptidases / Amyloid Precursor Protein Secretases Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Type: Article Affiliation country: Switzerland

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