Gamma secretase modulators: new Alzheimer's drugs on the horizon?
MG Bursavich, BA Harrison… - Journal of medicinal …, 2016 - ACS Publications
The rapidly aging population desperately requires new therapies for Alzheimer's disease.
Despite years of pharmaceutical research, limited clinical success has been realized, with …
Despite years of pharmaceutical research, limited clinical success has been realized, with …
Recent developments of small molecule γ-secretase modulators for Alzheimer's disease
S Mekala, G Nelson, YM Li - RSC Medicinal Chemistry, 2020 - pubs.rsc.org
Alzheimer's disease (AD) is the most common form of progressive neurodegenerative
disorder, marked by memory loss and a decline in cognitive function. The major hallmarks of …
disorder, marked by memory loss and a decline in cognitive function. The major hallmarks of …
Function and toxicity of amyloid beta and recent therapeutic interventions targeting amyloid beta in Alzheimer's disease
K Rajasekhar, M Chakrabarti… - Chemical …, 2015 - pubs.rsc.org
Amyloidogenesis has been implicated in a broad spectrum of diseases in which amyloid
protein is invariably misfolded and deposited in cells and organs. Alzheimer's disease is one …
protein is invariably misfolded and deposited in cells and organs. Alzheimer's disease is one …
APP substrate ectodomain defines amyloid‐β peptide length by restraining γ‐secretase processivity and facilitating product release
Sequential proteolysis of the amyloid precursor protein (APP) by γ‐secretases generates
amyloid‐β (Aβ) peptides and defines the proportion of short‐to‐long Aβ peptides, which is …
amyloid‐β (Aβ) peptides and defines the proportion of short‐to‐long Aβ peptides, which is …
Qualitative changes in human γ-secretase underlie familial Alzheimer's disease
M Szaruga, S Veugelen, M Benurwar… - Journal of Experimental …, 2015 - rupress.org
Presenilin (PSEN) pathogenic mutations cause familial Alzheimer's disease (AD [FAD]) in an
autosomal-dominant manner. The extent to which the healthy and diseased alleles influence …
autosomal-dominant manner. The extent to which the healthy and diseased alleles influence …
Extracellular interface between APP and Nicastrin regulates Aβ length and response to γ‐secretase modulators
D Petit, M Hitzenberger, S Lismont… - The EMBO …, 2019 - embopress.org
Abstract γ‐Secretase complexes (GSEC s) are multimeric membrane proteases involved in
a variety of physiological processes and linked to Alzheimer's disease (AD). Presenilin …
a variety of physiological processes and linked to Alzheimer's disease (AD). Presenilin …
Alzheimer's disease in people with Down's syndrome: the prospects for and the challenges of developing preventative treatments
P Castro, S Zaman, A Holland - Journal of neurology, 2017 - Springer
People with Down's syndrome (DS) are at high risk for developing Alzheimer's disease (AD)
at a relatively young age. This increased risk is not observed in people with intellectual …
at a relatively young age. This increased risk is not observed in people with intellectual …
Selective Buchwald–Hartwig arylation of C-amino-1, 2, 4-triazoles and other coordinating aminoheterocycles enabled by bulky NHC ligands and TPEDO activator
AV Astakhov, AY Chernenko, VV Kutyrev… - Inorganic Chemistry …, 2023 - pubs.rsc.org
C-Amino-1, 2, 4-triazoles are challenging polynitrogen substrates for metal-catalyzed
arylation due to their multidentate character, enhanced coordinating ability and decreased …
arylation due to their multidentate character, enhanced coordinating ability and decreased …
Enzyme–substrate interface targeting by imidazole‐based γ‐secretase modulators activates γ‐secretase and stabilizes its interaction with APP
D Petit, M Hitzenberger, M Koch, S Lismont… - The EMBO …, 2022 - embopress.org
Alzheimer's disease (AD) pathogenesis has been linked to the accumulation of longer,
aggregation‐prone amyloid β (Aβ) peptides in the brain. Γ‐secretases generate Aβ peptides …
aggregation‐prone amyloid β (Aβ) peptides in the brain. Γ‐secretases generate Aβ peptides …
Heterocyclic scaffolds for the treatment of Alzheimer's disease
A Martorana, V Giacalone, R Bonsignore… - Current …, 2016 - ingentaconnect.com
Background: The treatment and diagnosis of Alzheimer's Disease (AD) are two of the most
urgent goals for research around the world. The cognitive decline is generally associated …
urgent goals for research around the world. The cognitive decline is generally associated …