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Brian Clarke et al.
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Nicolas Charrier et al.
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
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Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
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Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4(phenylthio)butyric acid
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Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human β-secretase
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BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
Macrocyclic inhibitors of β-secretase:: Functional activity in an animal model
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
BACE-1 inhibition by a series of ψ[CH2NH] reduced amide isosteres
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human β-secretase inhibitors.: Design, synthesis, and enzymatic BACE-1 and cell assays
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
Design and synthesis of potent β-secretase (BACE1) inhibitors with P1′ carboxylic acid bioisosteres
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Design, synthesis and X-ray structure of protein-ligand complexes:: Important insight into selectivity of memapsin 2 (β-secretase) inhibitors
AK Ghosh et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2006)
In silico discovery of β-secretase inhibitors
DZ Huang et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2006)
BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles:: Chromene, coumarin and quinoline
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Cathepsin D is present in human eccrine sweat and involved in the postsecretory processing of the antimicrobial peptide DCD-1L
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JOURNAL OF BIOLOGICAL CHEMISTRY (2006)
Conformationally biased P3 amide replacements of β-secretase inhibitors
SJ Stachel et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): First X-ray structure of a macrocyclic peptidomimetic-BACE complex
I Rojo et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice
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JOURNAL OF NEUROCHEMISTRY (2006)
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold
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JOURNAL OF MEDICINAL CHEMISTRY (2005)
BACE1, a major determinant of selective vulnerability of the brain to amyloid-β amyloidogenesis, is essential for cognitive, emotional, and synaptic functions
FM Laird et al.
JOURNAL OF NEUROSCIENCE (2005)
Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics
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Discovery of cell-permeable non-peptide inhibitors of β-secretase by high-throughput docking and continuum electrostatics calculations
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JOURNAL OF MEDICINAL CHEMISTRY (2005)
Structural locations and functional roles of new subsites S5, S6, and S7 in memapsin 2 (β-secretase)
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BIOCHEMISTRY (2005)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2005)
Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability
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KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
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BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease
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Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
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Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase
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T Bussiere et al.
NEUROSCIENCE (2002)
The disulphide bonds in the catalytic domain of BACE are critical but not essential for amyloid precursor protein processing activity
F Fischer et al.
JOURNAL OF NEUROCHEMISTRY (2002)
Endosomal sorting of amyloid precursor protein-P-selectin chimeras influences secretase processing
BL Daugherty et al.
TRAFFIC (2001)
The β-secretase, BACE -: A prime drug target for Alzheimer's disease
R Vassar
JOURNAL OF MOLECULAR NEUROSCIENCE (2001)
Structure-based design:: Potent inhibitors of human brain memapsin 2 (β-secretase)
AK Ghosh et al.
JOURNAL OF MEDICINAL CHEMISTRY (2001)
Subsite specificity of memapsin 2 (β-secretase):: Implications for inhibitor design
RT Turner et al.
BIOCHEMISTRY (2001)
BACE knockout mice are healthy despite lacking the primary β-secretase activity in brain:: implications for Alzheimer's disease therapeutics
SL Roberds et al.
HUMAN MOLECULAR GENETICS (2001)
Post-translational processing of β-secretase (β-amyloid-converting enzyme) and its ectodomain shedding -: The pro- and transmembrane/cytosolic domains affect its cellular activity and amyloid-β production
S Benjannet et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2001)
The Pro domain of β-secretase does not confer strict zymogen-like properties but does assist proper folding of the protease domain
XP Shi et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2001)
Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation
Y Luo et al.
NATURE NEUROSCIENCE (2001)
BACE1 is the major β-secretase for generation of Aβ peptides by neurons
HB Cai et al.
NATURE NEUROSCIENCE (2001)
Presenilin-1 and-2 are molecular targets for γ-secretase inhibitors
D Seiffert et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2000)
Nonfibrillar diffuse amyloid deposition due to a γ42-secretase site mutation points to an essential role for N-truncated Aβ42 in Alzheimer's disease
S Kumar-Singh et al.
HUMAN MOLECULAR GENETICS (2000)
Maturation and endosomal targeting of β-site amyloid precursor protein-cleaving enzyme -: The Alzheimer's disease β-secretase
JT Huse et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2000)
Proteolytic activation of recombinant pro-memapsin 2 (pro-β-secretase) studied with new fluorogenic substrates
J Ermolieff et al.
BIOCHEMISTRY (2000)
Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor
L Hong et al.
SCIENCE (2000)
BACE2, a β-secretase homolog, cleaves at the β site and within the amyloid-β region of the amyloid-β precursor protein
M Farzan et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2000)
Characterization of Alzheimer's β-secretase protein BACE -: A pepsin family member with unusual properties
M Haniu et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2000)
Expression analysis of BACE2 in brain and peripheral tissues
BD Bennett et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2000)
Transition-state analogue inhibitors of γ-secretase bind directly to presenilin-1
WP Esler et al.
NATURE CELL BIOLOGY (2000)
Early-onset Alzheimer disease caused by a new mutation (V717L) in the amyloid precursor protein gene
JR Murrell et al.
ARCHIVES OF NEUROLOGY (2000)
Design of potent inhibitors for human brain memapsin 2 (β-secretase)
AK Ghosh et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2000)
Correlation between elevated levels of amyloid β-peptide in the brain and cognitive decline
J Näslund et al.
JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2000)
Human aspartic protease memapsin 2 cleaves the β-secretase site of β-amyloid precursor protein
XL Lin et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2000)
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