Secretase inhibitors and modulators for Alzheimer’s disease treatment

A helix-to-coil transition at the  -cut site in the transmembrane dimer of the amyloid precursor protein is required for proteolysis

(2009) T. Sato et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Orphan G Protein-Coupled Receptor 3 Modulates Amyloid-Beta Peptide Generation in Neurons

(2009) A. Thathiah et al.   SCIENCE

Design of Potent Aspartic Protease Inhibitors to Treat Various Diseases

(2008) Jeffrey-Tri Nguyen et al.   ARCHIV DER PHARMAZIE

Decrease in the Numbers of Dendritic Cells and CD4+ T Cells in Cerebral Perivascular Spaces Due to Natalizumab

(2008) Maria del Pilar Martin   ARCHIVES OF NEUROLOGY

Phase 2 Safety Trial Targeting Amyloid β Production With a γ-Secretase Inhibitor in Alzheimer Disease

(2008) Adam S. Fleisher et al.   ARCHIVES OF NEUROLOGY

Notch signaling and diseases: An evolutionary journey from a simple beginning to complex outcomes

(2008) Claudio Talora et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Discovery of a novel series of Notch-sparing γ-secretase inhibitors

(2008) Anthony Kreft et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Understanding BACE1: essential protease for amyloid-β production in Alzheimer’s disease

(2008) J. H. Stockley et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Substrate specificity of γ-secretase and other intramembrane proteases

(2008) A. J. Beel et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Part-Time α-Secretases: The Functional Biology of ADAM 9, 10 and 17

(2008) Miriam Deuss et al.   Current Alzheimer Research

Cancer Stem Cells: How can we Target them?

(2008) Ivan Ischenko et al.   CURRENT MEDICINAL CHEMISTRY

Core principles of intramembrane proteolysis: comparison of rhomboid and site-2 family proteases

(2008) S URBAN et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Therapeutic Potential of γ -Secretase Inhibitors and Modulators

(2008) Bruno Imbimbo   CURRENT TOPICS IN MEDICINAL CHEMISTRY

γ-secretase modulators: hopes and setbacks for the future of Alzheimer’s treatment

(2008) Genevieve Evin   Expert Review of Neurotherapeutics

Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves

(2008) Xiangyou Hu et al.   FASEB JOURNAL

Glu332in the Nicastrin Ectodomain Is Essential for γ-Secretase Complex Maturation but Not for Its Activity

(2008) Lucía Chávez-Gutiérrez et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Transmembrane Domain 9 of Presenilin Determines the Dynamic Conformation of the Catalytic Site of γ-Secretase

(2008) Alexandra Tolia et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Intramembrane Proteolysis of GXGD-type Aspartyl Proteases Is Slowed by a Familial Alzheimer Disease-like Mutation

(2008) Regina Fluhrer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Distinct Pharmacological Effects of Inhibitors of Signal Peptide Peptidase and γ-Secretase

(2008) Toru Sato et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

MicroRNA-298 and MicroRNA-328 Regulate Expression of Mouse β-Amyloid Precursor Protein-converting Enzyme 1

(2008) Vincent Boissonneault et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Role of Amyloid Precursor Protein Processing by BACE1, the β-Secretase, in Alzheimer Disease Pathophysiology

(2008) Sarah L. Cole et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Substrate Requirements for SPPL2b-dependent Regulated Intramembrane Proteolysis

(2008) Lucas Martin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Amyloidogenic Processing but Not Amyloid Precursor Protein (APP) Intracellular C-terminal Domain Production Requires a Precisely Oriented APP Dimer Assembled by Transmembrane GXXXG Motifs

(2008) Pascal Kienlen-Campard et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Amyloid Precursor Protein Trafficking, Processing, and Function

(2008) Gopal Thinakaran et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Membrane microdomain switching: a regulatory mechanism of amyloid precursor protein processing

(2008) Takashi Sakurai et al.   JOURNAL OF CELL BIOLOGY

Building γ-secretase – the bits and pieces

(2008) Dragana Spasic et al.   JOURNAL OF CELL SCIENCE

The molecular logic of Notch signaling - a structural and biochemical perspective

(2008) W. R. Gordon et al.   JOURNAL OF CELL SCIENCE

Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease

(2008) Scott C. Mayer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cryoelectron Microscopy Structure of Purified γ-Secretase at 12 Å Resolution

(2008) Pamela Osenkowski et al.   JOURNAL OF MOLECULAR BIOLOGY

Notch: from neural development to neurological disorders

(2008) Justin D. Lathia et al.   JOURNAL OF NEUROCHEMISTRY

Etazolate, a neuroprotective drug linking GABAAreceptor pharmacology to amyloid precursor protein processing

(2008) Maryline Marcade et al.   JOURNAL OF NEUROCHEMISTRY

Amyloid-  Peptide (A ) Neurotoxicity Is Modulated by the Rate of Peptide Aggregation: A  Dimers and Trimers Correlate with Neurotoxicity

(2008) L. W. Hung et al.   JOURNAL OF NEUROSCIENCE

The C-Terminal PAL Motif and Transmembrane Domain 9 of Presenilin 1 Are Involved in the Formation of the Catalytic Pore of the  -Secretase

(2008) C. Sato et al.   JOURNAL OF NEUROSCIENCE

The Expression of MicroRNA miR-107 Decreases Early in Alzheimer's Disease and May Accelerate Disease Progression through Regulation of  -Site Amyloid Precursor Protein-Cleaving Enzyme 1

(2008) W.-X. Wang et al.   JOURNAL OF NEUROSCIENCE

Crystal Structure of an Active Form of BACE1, an Enzyme Responsible for Amyloid   Protein Production

(2008) H. Shimizu et al.   MOLECULAR AND CELLULAR BIOLOGY

Therapeutic Strategies for Alzheimer’s Disease

(2008) Donna M. Barten et al.   MOLECULAR NEUROBIOLOGY

Substrate-targeting γ-secretase modulators

(2008) Thomas L. Kukar et al.   NATURE

Expression of a noncoding RNA is elevated in Alzheimer's disease and drives rapid feed-forward regulation of β-secretase

(2008) Mohammad Ali Faghihi et al.   NATURE MEDICINE

γ-secretase inhibitors reverse glucocorticoid resistance in T cell acute lymphoblastic leukemia

(2008) Pedro J Real et al.   NATURE MEDICINE

Thirty years of Alzheimer's disease genetics: the implications of systematic meta-analyses

(2008) Lars Bertram et al.   NATURE REVIEWS NEUROSCIENCE

Non-Cell-Autonomous Effects of Presenilin 1 Variants on Enrichment-Mediated Hippocampal Progenitor Cell Proliferation and Differentiation

(2008) Se Hoon Choi et al.   NEURON

Phosphorylation of the Translation Initiation Factor eIF2α Increases BACE1 Levels and Promotes Amyloidogenesis

(2008) Tracy O'Connor et al.   NEURON

Differential regulation of neurogenesis in two neurogenic regions of APPswe/PS1dE9 transgenic mice

(2008) Tetsuhiro Niidome et al.   NEUROREPORT

β-Secretase as a therapeutic target for Alzheimer’s disease

(2008) Arun K. Ghosh et al.   Neurotherapeutics

Inhibition and modulation of γ-secretase for Alzheimer’s disease

(2008) Michael S. Wolfe   Neurotherapeutics

Rational targeting of Notch signaling in cancer

(2008) P Rizzo et al.   ONCOGENE

Impaired Adult Neurogenesis in the Dentate Gyrus of a Triple Transgenic Mouse Model of Alzheimer's Disease

(2008) José J. Rodríguez et al.   PLoS One

Deficiency of Aph1B/C- -secretase disturbs Nrg1 cleavage and sensorimotor gating that can be reversed with antipsychotic treatment

(2008) T. Dejaegere et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Loss of microRNA cluster miR-29a/b-1 in sporadic Alzheimer's disease correlates with increased BACE1/ -secretase expression

(2008) S. S. Hebert et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Alteration of BACE1-dependent NRG1/ErbB4 signaling and schizophrenia-like phenotypes in BACE1-null mice

(2008) A. V. Savonenko et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Presenilin: RIP and beyond

(2008) Matthew R. Hass et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

The “A Disintegrin And Metalloprotease” (ADAM) family of sheddases: Physiological and cellular functions

(2008) Karina Reiss et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Proteomic Profiling of γ-Secretase Substrates and Mapping of Substrate Requirements

(2008) Matthew L Hemming et al.   PLOS BIOLOGY

Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

(2007) Derek C. Cole et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent memapsin 2 (β-secretase) inhibitors: Design, synthesis, protein-ligand X-ray structure, and in vivo evaluation

(2007) Arun K. Ghosh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

BACE1 gene deletion: Impact on behavioral function in a model of Alzheimer's disease

(2007) Dione Kobayashi et al.   NEUROBIOLOGY OF AGING