AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics
出版年份 2016 全文链接
标题
AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics
作者
关键词
-
出版物
JOURNAL OF ALZHEIMERS DISEASE
Volume 50, Issue 4, Pages 1109-1123
出版商
IOS Press
发表日期
2016-02-24
DOI
10.3233/jad-150834
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design
- (2015) Christopher R. Butler et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central A Pharmacodynamic Responses in Mice, Dogs, and Humans
- (2015) P. C. May et al. JOURNAL OF NEUROSCIENCE
- The Structural Evolution of β-Secretase Inhibitors: A Focus on the Development of Small-Molecule Inhibitors
- (2014) Stefania Butini et al. CURRENT TOPICS IN MEDICINAL CHEMISTRY
- Molecular Mechanisms of Alzheimer Disease Protection by the A673T Allele of Amyloid Precursor Protein
- (2014) Janice A. Maloney et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Revisiting the peripheral sink hypothesis: inhibiting BACE1 activity in the periphery does not alter β-amyloid levels in the CNS
- (2014) Biljana Georgievska et al. JOURNAL OF NEUROCHEMISTRY
- CNS Amyloid- , Soluble APP- and - Kinetics during BACE Inhibition
- (2014) J. A. Dobrowolska et al. JOURNAL OF NEUROSCIENCE
- BACE1 inhibitor drugs in clinical trials for Alzheimer’s disease
- (2014) Robert Vassar Alzheimers Research & Therapy
- β-secretase inhibitor; a promising novel therapeutic drug in Alzheimer’s disease
- (2014) Kelly Willemijn Menting et al. Frontiers in Aging Neuroscience
- Sustained peripheral depletion of amyloid-β with a novel form of neprilysin does not affect central levels of amyloid-β
- (2013) Simon J. Henderson et al. BRAIN
- AZ-4217: A High Potency BACE Inhibitor Displaying Acute Central Efficacy in Different In Vivo Models and Reduced Amyloid Deposition in Tg2576 Mice
- (2013) S. Eketjall et al. JOURNAL OF NEUROSCIENCE
- Population PKPD Modeling of BACE1 Inhibitor-Induced Reduction in Aβ Levels In Vivo and Correlation to In Vitro Potency in Primary Cortical Neurons from Mouse and Guinea Pig
- (2013) Juliette Janson et al. PHARMACEUTICAL RESEARCH
- Discovery of AZD3839, a Potent and Selective BACE1 Inhibitor Clinical Candidate for the Treatment of Alzheimer Disease
- (2012) Fredrik Jeppsson et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- New Aminoimidazoles as β-Secretase (BACE-1) Inhibitors Showing Amyloid-β (Aβ) Lowering in Brain
- (2012) Ylva Gravenfors et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure- and Property-Based Design of Aminooxazoline Xanthenes as Selective, Orally Efficacious, and CNS Penetrable BACE Inhibitors for the Treatment of Alzheimer’s Disease
- (2012) Hongbing Huang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design and Synthesis of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β-Amyloid Peptides
- (2012) Britt-Marie Swahn et al. JOURNAL OF MEDICINAL CHEMISTRY
- Alzheimer's Disease: Presenilin 2-Sparing -Secretase Inhibition Is a Tolerable A Peptide-Lowering Strategy
- (2012) T. Borgegard et al. JOURNAL OF NEUROSCIENCE
- A mutation in APP protects against Alzheimer’s disease and age-related cognitive decline
- (2012) Thorlakur Jonsson et al. NATURE
- Robust Central Reduction of Amyloid- in Humans with an Orally Available, Non-Peptidic -Secretase Inhibitor
- (2011) P. C. May et al. JOURNAL OF NEUROSCIENCE
- The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics
- (2011) Eric Karran et al. NATURE REVIEWS DRUG DISCOVERY
- Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System
- (2009) M. Friden et al. DRUG METABOLISM AND DISPOSITION
- Application of a Dried-DMSO rapid throughput 24-h equilibrium solubility in advancing discovery candidates
- (2009) Yun W. Alelyunas et al. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
- Extensions to the Visual Predictive Check to facilitate model performance evaluation
- (2008) Teun M. Post et al. JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS
- First Demonstration of Cerebrospinal Fluid and Plasma A Lowering with Oral Administration of a -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates
- (2008) S. Sankaranarayanan et al. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Become a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get StartedAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started