Results 181 to 190 of about 27,905 (224)
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Delta- and beta- secretases crosstalk amplifies the amyloidogenic pathway in Alzheimer’s disease
Progress in Neurobiology, 2021Asparagine endopeptidase (AEP), a newly identified delta-secretase, simultaneously cleaves both APP and Tau, promoting Alzheimer's disease (AD) pathologies. However, its pathological role in AD remains incompletely understood. Here we show that delta-secretase cleaves BACE1, a rate-limiting protease in amyloid-β (Aβ) generation, escalating its ...
Yiyuan Xia +7 more
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Screening of Beta-Secretase Inhibitors by Capillary Electrophoresis-Mass Spectrometry
2019Alzheimer's disease is the most common cause of dementia, currently afflicting almost 40 million patients worldwide. According to the amyloid cascade hypothesis, the pathogenesis of the disease could be slowed down or even stopped by the inhibition of beta-secretase, making this aspartic acid protease a potentially important drug target site. Capillary
Jan, Schejbal +2 more
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Journal of Neuroscience Research, 2004
AbstractThe β‐amyloid peptides derived by proteolytic cleavage from the amyloid precursor protein (APP) play a major role in the pathogenesis of Alzheimer's disease (AD) by forming aggregated, fibrillary complexes that have been shown to be neurotoxic.
Thole, Züchner +2 more
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AbstractThe β‐amyloid peptides derived by proteolytic cleavage from the amyloid precursor protein (APP) play a major role in the pathogenesis of Alzheimer's disease (AD) by forming aggregated, fibrillary complexes that have been shown to be neurotoxic.
Thole, Züchner +2 more
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Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors
Bioorganic & Medicinal Chemistry, 2017Taking advantage of the structural similarity between aspartic proteases, small-molecule peptidomimetic inhibitors that already showed activity towards Secreted Aspartic Protease 2 as anti-Candida agents and HIV protease inhibitors were exploited as potential BACE1 inhibitors.
INNOCENTI, RICCARDO +4 more
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beta-Secretase, APP and Abeta in Alzheimer's disease.
Sub-cellular biochemistry, 2005Amyloid plaques, hallmark neuropathological lesions in Alzheimer's disease (AD) brain, are composed of the beta-amyloid peptide (Abeta). A large body of evidence suggests Abeta is central to the pathophysiology of AD and is likely to start this intractable neurodegenerative disorder. Mutations in three genes (amyloid precursor protein/APP, presenilin1,
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Abstract WP555: Plasma Beta-Secretase 1 in Cerebral Amyloid Angiopathy
Stroke, 2019Backgrouds: Beta-secretase 1 (BACE1) is the rate-limiting enzyme in amyloidogenesis. We have recently reported that plasma BACE1 activity may predict Alzheimer’s disease as surrogate biomarkers, and BACE1 protein and activity levels are increased in cortical vessels from patients with cerebral amyloid angiopathy (CAA). However,
Ya Su +4 more
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2D QSAR Studies on Series of Human Beta-secretase (BACE-1) Inhibitors
Medicinal Chemistry, 2014β-secretase (BACE-1) plays a pivotal role in the β-Amyloid plaques formation, which is responsible for progressive cognitive and memory loss commonly found in Alzheimer disease patients. As a consequence, it has been considered as a good target for drug development efforts.
Daniela Santos, Cruz +1 more
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Modulators and inhibitors of gamma- and beta-secretases.
Neuro-degenerative diseases, 2006Most gene mutations associated with Alzheimer's disease point to the metabolism of amyloid precursor protein as a potential cause. The beta- and gamma-secretases are two executioners of amyloid precursor protein processing resulting in amyloid-beta.
Boris, Schmidt +4 more
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In Silico Design of Beta‐Secretase Inhibitors in Alzheimer's Disease
Chemical Biology & Drug Design, 2014Alzheimer's disease is the major cause of senile dementia, flewing out 10% of 65 years old and 50% of 85 years old global population. The major fisiopathologic characteristics of Alzheimer's disease are the deposition of extracellular neuritic plaques and the presence of intracellular neurofibrillary tangles in memory‐related areas of the brain.
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Serotonin derivatives as inhibitors of beta-secretase (BACE 1).
Die Pharmazie, 2011All serotonin derivatives described here (1-9) inhibited BACE 1 in a dose dependent manner. The 50% Inhibition Concentration (IC50) of N-cinnamoyl serotonin (1) was 86.7 +/- 4.0 microM. The peptide conjugation of serotonin derivatives influenced the BACE 1 inhibitory activity.
T, Takahashi, M, Miyazawa
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