نتایج جستجو برای: bace 1
تعداد نتایج: 2752751 فیلتر نتایج به سال:
OBJECTIVE The purpose of this study was to investigate the effects and pharmacological mechanisms of icariin, which is the main component in the traditional Chinese herb Epimedium, on β-amyloid (Aβ) production in an amyloid precursor protein (APP) transgenic (Tg) mouse model of Alzheimer's disease (AD). METHODS APPV717I Tg mice were randomly divided into a model group and icariin-treated (30 ...
beta-Secretase (BACE) is a membrane-bound aspartyl protease that cleaves the amyloid precursor protein to generate the N terminus of the amyloid beta peptide. BACE is expressed as a precursor protein containing Pre, Pro, protease, transmembrane, and cytosolic domains. A soluble BACE derivative (PreProBACE460) that is truncated between the protease and transmembrane domains was produced by bacul...
Cerebral deposition of amyloid beta peptide (Abeta) is an early and critical feature of Alzheimer's disease. Abeta generation depends on proteolytic cleavage of the amyloid precursor protein (APP) by two unknown proteases: beta-secretase and gamma-secretase. These proteases are prime therapeutic targets. A transmembrane aspartic protease with all the known characteristics of beta-secretase was ...
The possibility of an express assessment of quality medicinal raw materials Rhaponticum carthamoides (Willd.) Iljin is investigated, at various stages of harvesting and storage by method Bromic Antioxidant Capacity Estimation (BACE), after extraction of sample in an aqueous solution. Revealed that phytoecdysteroids R. carthamoides extracted in aqueous solution at level of ethanol, have the temp...
The thermodynamic, kinetic, and structural properties of Ln3+ complexes with the bifunctional DO3A-ACE4? ligand its amide derivative DO3A-BACE4? (modelling case where binds to vector molecules) have been studied in order confirm usefulness corresponding Gd3+ as relaxation labels targeted MRI contrast agents. stability constants Mg2+ Ca2+ are lower than for DOTA4? DO3A3?, while Zn2+ Cu2+ similar...
A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic and cell-based assays, were observed in this series of target compounds, with the best candidates displaying cell-based IC(50) values in the low...
β-Secretase (BACE-1) constitutes an important target for search of anti-Alzheimer's drugs. The first inhibitors of this enzyme were peptidic compounds with high molecular weight and low bioavailability. Therefore, the search for new efficient non-peptidic inhibitors has been undertaken by many scientific groups. We started our work from the development of in silico methodology for the design of...
Fragile X syndrome (FXS) is a debilitating genetic disorder with no cure and few therapeutic options. Excessive signaling through metabotropic glutamate receptor 5 in FXS leads to increased translation of numerous synaptic proteins and exaggerated long-term depression. Two of the overexpressed proteins are amyloid-beta protein precursor (APP) and its metabolite amyloid-beta, which have been wel...
Our research has concentrated upon the protein lipid modification of BACE [beta-site amyloid precursor protein cleaving enzyme (beta-secretase)], of which very little is currently known. Lipidation influences the production of Abeta (amyloid beta-protein) by promoting the dimerization of BACE.
CONTEXT Amyloid plaques, a major pathological feature of Alzheimer disease (AD), are composed of an internal fragment of amyloid precursor protein (APP): the 4-kd amyloid-beta protein (Abeta). The metabolic processing of APP that results in Abeta formation requires 2 enzymatic cleavage events, a gamma-secretase cleavage dependent on presenilin, and a beta-secretase cleavage by the aspartyl prot...
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