A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.

Hills, Ivory D; Holloway, M Katharine; de León, Pablo; Nomland, Ashley; Zhu, Hong; Rajapakse, Hemaka; Allison, Tim J; Munshi, Sanjeev K; Colussi, Dennis; Pietrak, Beth L; Toolan, Dawn; Haugabook, Sharie J; Graham, Samuel L; Stachel, Shawn J

Hills, Ivory D; Holloway, M Katharine; de León, Pablo; Nomland, Ashley; Zhu, Hong; Rajapakse, Hemaka; Allison, Tim J; Munshi, Sanjeev K; Colussi, Dennis; Pietrak, Beth L; Toolan, Dawn; Haugabook, Sharie J; Graham, Samuel L; Stachel, Shawn J.

Affiliation

Hills ID; Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., West Point, PA 19486, USA. ivory_hills@merck.com

Bioorg Med Chem Lett ; 19(17): 4993-5, 2009 Sep 01.

Article in En | MEDLINE | ID: mdl-19640712

Subject(s)

Amyloid Precursor Protein Secretases/antagonists & inhibitors; Imidazoles/chemistry; Protease Inhibitors/chemistry; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism; Amyloid Precursor Protein Secretases/metabolism; Binding Sites; Catalytic Domain; Crystallography, X-Ray; Drug Design; Humans; Imidazoles/chemical synthesis; Imidazoles/pharmacology; Molecular Conformation; Protease Inhibitors/chemical synthesis; Protease Inhibitors/pharmacology; Protein Structure, Tertiary

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protease Inhibitors / Amyloid Precursor Protein Secretases / Imidazoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country: United States Country of publication: United kingdom

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