Inhibition of γ-Secretase Leads to an Increase in Presenilin-1

Intraneuronal aggregation of the β-CTF fragment of APP (C99) induces Aβ-independent lysosomal-autophagic pathology

(2016) Inger Lauritzen et al.   ACTA NEUROPATHOLOGICA

Restricted Location of PSEN2/γ-Secretase Determines Substrate Specificity and Generates an Intracellular Aβ Pool

(2016) Ragna Sannerud et al.   CELL

Alzheimer's disease

(2016) Philip Scheltens et al.   LANCET

Cerebrospinal fluid Presenilin-1 increases at asymptomatic stage in genetically determined Alzheimer’s disease

(2016) Aitana Sogorb-Esteve et al.   Molecular Neurodegeneration

Learning by Failing: Ideas and Concepts to Tackle γ-Secretases in Alzheimer's Disease and Beyond

(2015) Bart De Strooper et al.   Annual Review of Pharmacology and Toxicology

Complex regulation of γ-secretase: from obligatory to modulatory subunits

(2015) Natalya Gertsik et al.   Frontiers in Aging Neuroscience

Amyloid β-protein oligomers upregulate the β-secretase, BACE1, through a post-translational mechanism involving its altered subcellular distribution in neurons

(2015) Naomi Mamada et al.   Molecular Brain

Targeting Prodromal Alzheimer Disease With Avagacestat

(2015) Vladimir Coric et al.   JAMA Neurology

Lessons from a BACE1 inhibitor trial: Off-site but not off base

(2014) Debomoy K. Lahiri et al.   Alzheimers & Dementia

Lessons from a Failed γ-Secretase Alzheimer Trial

(2014) Bart De Strooper   CELL

Physiological Functions of Presenilins; Beyond γ-Secretase

(2014) Ibolya Stiller et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

Clinical trials and late-stage drug development for Alzheimer's disease: an appraisal from 1984 to 2014

(2014) L. S. Schneider et al.   JOURNAL OF INTERNAL MEDICINE

Interpreting Alzheimer’s disease clinical trials in light of the effects on amyloid-β

(2014) Jeremy H Toyn et al.   Alzheimers Research & Therapy

Multi-target action of the novel anti-Alzheimer compound CHF5074: in vivo study of long term treatment in Tg2576 mice

(2013) Sandra Sivilia et al.   BMC NEUROSCIENCE

Age-related neuropsychiatric symptoms in presenilins conditional double knockout mice

(2013) Li Yan et al.   BRAIN RESEARCH BULLETIN

ApoER2 processing by presenilin-1 modulates reelin expression

(2013) Valeria Balmaceda et al.   FASEB JOURNAL

Potential novel targets for Alzheimer pharmacotherapy: II. Update on secretase inhibitors and related approaches

(2013) J. A. Mikulca et al.   JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS

Targeting Notch signaling pathway in cancer: Clinical development advances and challenges

(2013) Naoko Takebe et al.   PHARMACOLOGY & THERAPEUTICS

Presenilins and  -Secretase: Structure, Function, and Role in Alzheimer Disease

(2013) B. De Strooper et al.   Cold Spring Harbor Perspectives in Medicine

Trafficking and Proteolytic Processing of APP

(2013) C. Haass et al.   Cold Spring Harbor Perspectives in Medicine

CSF Presenilin-1 complexes are increased in Alzheimer’s disease

(2013) María-Salud García-Ayllón et al.   Acta Neuropathologica Communications

Safety and Tolerability of the γ-Secretase Inhibitor Avagacestat in a Phase 2 Study of Mild to Moderate Alzheimer Disease

(2012) Vladimir Coric et al.   ARCHIVES OF NEUROLOGY

Effects of Single Doses of Avagacestat (BMS-708163) on Cerebrospinal Fluid Aβ Levels in Healthy Young Men

(2012) Gary Tong et al.   CLINICAL DRUG INVESTIGATION

A Placebo-Controlled, Multiple Ascending Dose Study to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of Avagacestat (BMS-708163) in Healthy Young and Elderly Subjects

(2012) Randy Dockens et al.   CLINICAL PHARMACOKINETICS

Multicenter, Randomized, Double-Blind, Placebo-Controlled, Single-Ascending Dose Study of the Oral γ-Secretase Inhibitor BMS-708163 (Avagacestat): Tolerability Profile, Pharmacokinetic Parameters, and Pharmacodynamic Markers

(2012) Gary Tong et al.   CLINICAL THERAPEUTICS

The mechanism of γ-Secretase dysfunction in familial Alzheimer disease

(2012) Lucía Chávez-Gutiérrez et al.   EMBO JOURNAL

Differential Effects between  -Secretase Inhibitors and Modulators on Cognitive Function in Amyloid Precursor Protein-Transgenic and Nontransgenic Mice

(2012) Y. Mitani et al.   JOURNAL OF NEUROSCIENCE

The  -Secretase-Derived C-Terminal Fragment of  APP, C99, But Not A , Is a Key Contributor to Early Intraneuronal Lesions in Triple-Transgenic Mouse Hippocampus

(2012) I. Lauritzen et al.   JOURNAL OF NEUROSCIENCE

Association of Existing and New Candidate Genes for Anxiety, Depression and Personality Traits in Older People

(2010) Michelle Luciano et al.   BEHAVIOR GENETICS

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor

(2010) Kevin W. Gillman et al.   ACS Medicinal Chemistry Letters

A novel Aβ isoform pattern in CSF reflects γ-secretase inhibition in Alzheimer disease

(2010) Erik Portelius et al.   Alzheimers Research & Therapy

Chronic Administration of KB-R7943 Induces Up-regulation of Cardiac NCX1

(2009) Lin Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The  -Secretase Enzyme BACE in Health and Alzheimer's Disease: Regulation, Cell Biology, Function, and Therapeutic Potential

(2009) R. Vassar et al.   JOURNAL OF NEUROSCIENCE

Begacestat (GSI-953): A Novel, Selective Thiophene Sulfonamide Inhibitor of Amyloid Precursor Protein  -Secretase for the Treatment of Alzheimer's Disease

(2009) R. L. Martone et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A novel pathway for amyloid precursor protein processing

(2009) Erik Portelius et al.   NEUROBIOLOGY OF AGING

Reduced anxiety in the mice expressing mutant (N141I) presenilin 2

(2008) Dong Yeon Yuk et al.   JOURNAL OF NEUROSCIENCE RESEARCH

Presenilin 1 Interacts with Acetylcholinesterase and Alters Its Enzymatic Activity and Glycosylation

(2008) M.-X. Silveyra et al.   MOLECULAR AND CELLULAR BIOLOGY

Presenilins: Members of the γ-Secretase Quartets, But Part-Time Soloists Too

(2008) Tomoko Wakabayashi et al.   PHYSIOLOGY

Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain

(2003) H. F. Dovey et al.   JOURNAL OF NEUROCHEMISTRY