From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)
about
Computational approaches in target identification and drug discoveryComputational Insights into Substrate and Site Specificities, Catalytic Mechanism, and Protonation States of the Catalytic Asp Dyad of β -SecretaseSimplified 2-Aminoquinoline-Based Scaffold for Potent and Selective Neuronal Nitric Oxide Synthase InhibitionHitting the target: fragment screening with acoustic in situ co-crystallization of proteins plus fragment libraries on pin-mounted data-collection micromeshes.BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's diseaseAmyloid-beta: a crucial factor in Alzheimer's disease.Fragment-based drug discovery using a multidomain, parallel MD-MM/PBSA screening protocol.Monitoring β-secretase activity in living cells with a membrane-anchored FRET probe.Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011).Advances in the identification of β-secretase inhibitors.The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.NSAID-based γ-secretase modulators do not bind to the amyloid-β polypeptide.Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin.Cyanoacetamides (IV): versatile one-pot route to 2-quinoline-3-carboxamides.An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.Tandem Cu-catalyzed ketenimine formation and intramolecular nucleophile capture: Synthesis of 1,2-dihydro-2-iminoquinolines from 1-(o-acetamidophenyl)propargyl alcoholsNitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors.Mesenchymal stem cell-derived extracellular vesicles: a glimmer of hope in treating Alzheimer's disease.Recent advances in transition-metal-catalyzed reactions of alkynes with isoxazoles.Effect of sampling on BACE-1 ligands binding free energy predictions via MM-PBSA calculations.Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment.Copper-catalyzed synthesis of quinoline derivatives via tandem Knoevenagel condensation, amination and cyclization
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P2860
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)
description
2011 nî lūn-bûn
@nan
2011 թուականի Օգոստոսին հրատարակուած գիտական յօդուած
@hyw
2011 թվականի օգոստոսին հրատարակված գիտական հոդված
@hy
2011年の論文
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2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
name
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
@ast
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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type
label
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
@en
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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prefLabel
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
@ast
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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P2093
P3181
P356
P1476
From fragment screening to in ...... tein cleaving enzyme 1 (BACE1)
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P2093
Brad Jordan
Claire Rattan
David J St Jean
Dean Hickman
James Brown
Klaus Michelsen
Michael D Bartberger
Patricia Lopez
Paul H Wen
P304
P3181
P356
10.1021/JM200544Q
P407
P577
2011-07-29T00:00:00Z