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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2010-7-16
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ClarkeBrianB,
pubmed-author:CutlerLeanneL,
pubmed-author:DemontEmmanuelE,
pubmed-author:DingwallColinC,
pubmed-author:DunsdonRachelR,
pubmed-author:HawkinsJulieJ,
pubmed-author:HowesColinC,
pubmed-author:HussainIshrutI,
pubmed-author:MaileGrahamG,
pubmed-author:MaticoRosalieR,
pubmed-author:MosleyJulieJ,
pubmed-author:NaylorAlanA,
pubmed-author:O'BrienAlistairA,
pubmed-author:RedshawSallyS,
pubmed-author:RowlandPaulP,
pubmed-author:SmithKathrine JKJ,
pubmed-author:SoleilVirginieV,
pubmed-author:SweitzerSharonS,
pubmed-author:TheobaldPamP,
pubmed-author:VeseyDavidD,
pubmed-author:WalterDaryl SDS,
pubmed-author:WayneGarethG
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4639-44
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pubmed:meshHeading |
pubmed-meshheading:20579874-Alzheimer Disease,
pubmed-meshheading:20579874-Amyloid Precursor Protein Secretases,
pubmed-meshheading:20579874-Animals,
pubmed-meshheading:20579874-Arginine,
pubmed-meshheading:20579874-Binding Sites,
pubmed-meshheading:20579874-Computer Simulation,
pubmed-meshheading:20579874-Crystallography, X-Ray,
pubmed-meshheading:20579874-Ethylamines,
pubmed-meshheading:20579874-Protease Inhibitors,
pubmed-meshheading:20579874-Rats,
pubmed-meshheading:20579874-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
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pubmed:affiliation |
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, New Frontiers Science Park, Harlow, Essex, UK.
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pubmed:publicationType |
Journal Article
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