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Gamma-Secretase Inhibitors Relocate Presenilin1/gamma-Secretase to Late Endosomes/Lysosomes
Sannerud, R. +7 more
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Mechanism of gamma‐secretase modulators
Alzheimer's & Dementia, 2022AbstractBackgroundAmyloid‐beta (Aβ) peptides are believed to be integral to Alzheimer’s disease (AD) pathogenesis through their role in the “amyloid hypothesis,” in which the accumulation of Aβ peptides initiates a cascade of pathological events leading to neurodegeneration and AD.
Joanna E. Luo +2 more
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Biochemical Society transactions, 2003
Development of Alzheimer's disease (AD) pathology appears to be causally related to age-dependent changes in the metabolism of the amyloid-beta peptide (A beta), leading to its enhanced aggregation and deposition. gamma-Secretase is a crucial enzyme for the generation of A beta from the amyloid-beta precursor protein and thus represents a valid ...
D, Beher, M S, Shearman
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Development of Alzheimer's disease (AD) pathology appears to be causally related to age-dependent changes in the metabolism of the amyloid-beta peptide (A beta), leading to its enhanced aggregation and deposition. gamma-Secretase is a crucial enzyme for the generation of A beta from the amyloid-beta precursor protein and thus represents a valid ...
D, Beher, M S, Shearman
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Relationship between presenilinase and gamma-secretase
Drug News & Perspectives, 2003Genetic and neuropathological studies suggest that processing of amyloid precursor protein (APP) to yield amyloid beta-protein (Abeta) plays an important role in the pathogenesis of Alzheimer's disease (AD). One of the current therapeutic efforts for AD is directed towards blocking the gamma-secretase activity that produces Abeta.
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Gamma secretase inhibitors: a patent review (2013 - 2015)
Expert Opinion on Therapeutic Patents, 2017Gamma secretase (GS) is an intricate and multi-subunits complex, and it can cut various transmembrane proteins. Now it is a therapeutic target for a number of diseases. However, due to some side effects, the clinical development of GSI is not successful. Therefore, searching for effective GSIs has become a key point in drug discovery.
Kai, Gu +8 more
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Design and optimization of tricyclic gamma-secretase modulators
Bioorganic & Medicinal Chemistry Letters, 2016Beginning with a diaminotriazine screening hit, several series of novel, tricyclic gamma-secretase modulators (GSMs) were designed. The SAR of several related series of GSMs is presented, and the in vivo profile of a lead molecule from the series is described.
Jianliang, Shi +8 more
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Gamma-secretase: never more enigmatic.
Trends in neurosciences, 2002It is widely believed that the pathogenesis of Alzheimer's disease (AD) is intimately, if not causatively, associated with the deposition of approximately 4 kDa beta-amyloid (A beta) peptides in the cerebral cortex and hippocampus of affected individuals. A beta peptides are liberated from transmembrane proteins, termed beta-amyloid precursor proteins (
S S, Sisodia +3 more
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Current Alzheimer research, 2005
Accumulation of the amyloid beta-peptide (Abeta) in the brain is believed to initiate a series of neurotoxic events that causes neurodegeneration in Alzheimer's disease (AD). Abeta is generated by processing of the beta-amyloid precursor protein (APP) through the successive action of two proteolytic enzymes, beta-secretase and gamma-secretase.
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Accumulation of the amyloid beta-peptide (Abeta) in the brain is believed to initiate a series of neurotoxic events that causes neurodegeneration in Alzheimer's disease (AD). Abeta is generated by processing of the beta-amyloid precursor protein (APP) through the successive action of two proteolytic enzymes, beta-secretase and gamma-secretase.
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Current Alzheimer research, 2008
gamma-Secretase is responsible for the final cut of the amyloid beta-peptide (Abeta) precursor (APP) to produce the Abeta peptide implicated the pathogenesis of Alzheimer's disease (AD). Thus, this protease is a top target for the development of AD therapeutics.
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gamma-Secretase is responsible for the final cut of the amyloid beta-peptide (Abeta) precursor (APP) to produce the Abeta peptide implicated the pathogenesis of Alzheimer's disease (AD). Thus, this protease is a top target for the development of AD therapeutics.
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Rinsho shinkeigaku = Clinical neurology, 2007
Deposition of amyloid beta peptides (Abeta) as amyloid deposits characterizes the brains of patients with Alzheimer's disease (AD). Mutations in presenilin genes linked to familial AD (FAD) have been shown to increase production of Abeta42, an initially and predominantly depositing Abeta species in all types of AD.
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Deposition of amyloid beta peptides (Abeta) as amyloid deposits characterizes the brains of patients with Alzheimer's disease (AD). Mutations in presenilin genes linked to familial AD (FAD) have been shown to increase production of Abeta42, an initially and predominantly depositing Abeta species in all types of AD.
openaire +1 more source