分泌酶

AD治疗新药物&γ-分泌酶抑制剂

Promising drugs to treat Alzheimers disease & γ - secretase inhibitors

γ-分泌酶抑制剂能抑制A2780细胞的增殖，使细胞克隆形成率下降（p0.001）。

Cloning experiment presumed that γ - secretase inhibitors can inhibit the proliferation of A2780 cells , and the cell colony formation rate decreased ( p 0.001 ) . 4 .

选择性抑制γ-分泌酶的活性是抗AD药物研发中面临的一大挑战。

The selective inhibition of γ - secretase is a challenge in the development of anti-AD drugs .

【结论】1.γ-分泌酶抑制剂能够抑制A2780细胞的生长及增殖。

【 Conclusion 】 1 . γ - secretase inhibitors can inhibit cell growth and proliferation of A2780 .

目的观察中药新复方参乌胶囊对β-淀粉样肽前体蛋白（APP）转基因小鼠脑内β-淀粉样肽（Aβ）代谢及β-和γ-分泌酶的影响。

Objective To investigate the effects of Chinese herb compound Shen-wu capsule on the metabolism of β - amyloid ( A β) and β - and γ - secretase in β - amyloid precursor protein ( APP ) transgenic mice .

近年来很多研究都集中在α、β和γ-分泌酶对APP的作用和Aβ生成的影响上，以及家族性ADFAD和散发性ADSAD的发病原因和进程的研究。

In recent years , studies have focused on understanding the generation of A β peptides by the α - , β - and γ - secretase activity on APP , as cause and progression of both familial and sporadic AD ( FAD and SAD ) .

随着对AD分子和细胞病理生理的进一步了解，又发展了医一些新的治疗方法，如分泌酶抑制剂、过渡金属元素螯合剂、HMGCoA还原酶抑制剂和β淀粉样蛋白疫苗等。

Recent progress in understanding the molecular and cellular pathophysiology of Alzheimer 's disease has suggested possible pharmacological interventions , such as treatment with secretase inhibitors , transition metal chelators , HMG-CoA reductase inhibitors and amyloid - β immunization .

进一步的研究表明，由forskolin激活的CREB显著地促进PEN-2mRNA和蛋白质的表达，而对γ-分泌酶的其他组分没有影响。

Furthermore , activation of CREB by forskolin treatment dramatically promoted the expression of PEN-2 mRNA and protein , but not the expression of the other three γ - secretase components .

结果PS1M146L/APP（751），双转染CHO细胞系与野生型PS1/APP（751）双转染CHO细胞系相比α-分泌酶活性有降低，统计学检验差异显著（P＜<0.05）。

Results The α - secretase activity was decreased with a significant difference statistically ( P < 0.05 ) after the comparison between the double transfected stable expressions of CHO cell lines in PS1M146L / APP_ ( 751 ) and wild-type PS1 / APP_ ( 751 ) .

目的构建APP751和PS1（M146L）双重基因稳定转染的中国仓鼠卵巢（CHO）细胞系，以用于β分泌酶或γ分泌酶抑制剂的研究和相关药物的筛选。

AIM To study pathogenesis of Alzheimers disease and screen β - secretase and γ - secretase inhibiting drug , PS-1 ( M 146L ) and APP 751 gene double stably transfected CHO cell lines have been established .

γ分泌酶由四种组分PS、Aph-1、NCT及Pen-2构成，由于该酶的相对分子质量巨大以及结构复杂，所以研究进展比较缓慢，其结构与功能至今仍未完全揭示。

γ - secretase consists of four components PS , Aph-1 , NCT and Pen-2.Researching progress about this enzyme is slowly and its structure and function are not entirely understood by far because of its high molecular weight and complicated complex structure .

阿尔茨海默病与淀粉样β分泌酶基因的相关性研究

Amyloid β secretase gene and the risk for Alzheimer 's disease

β分泌酶抑制剂体外筛选模型的构建与验证

A screen assay of β - secretase inhibitors in vitro

Nicastrin：一种新型的γ-分泌酶组成蛋白

Nicastrin : a New Protein Component of γ - Secretase

β-分泌酶在脑淀粉样血管病变中的作用研究

Roles of β - secretase in the Pathogenesis of Cerebral Amyloid Angiopathy

α分泌酶在阿尔茨海默病治疗中的作用

Therapeutic Potential of α - Secretase in Alzheimer 's Disease

治疗阿尔采末病的药物靶点：β-分泌酶

A drug target for Alzheimers disease : β - secretase

新型γ-分泌酶抑制剂的设计与合成

Design and Synthesis of New γ - Secretase Inhibitors

与老年性痴呆相关分泌酶基因的转录调控

Transcriptional Regulation of Secretase Genes in Alzheimer 's Disease

这一作用在γ分泌酶抑制剂的处理结果中得到了证实。

This conclusion can be also demonstrated in γ secretase inhibitor treatment experiment .

γ-分泌酶在神经干细胞分化过程中的调节作用

Regulatory effects of gamma-secretase in neural stem cell differentiation

γ-分泌酶抑制剂的药效团模型构建

Pharmacophore Model Construction of γ - secretase Inhibitor

目的深入探讨基于羟基亚乙基二肽的β-分泌酶抑制剂的合成方法。

Aim To discuss in depth the synthesis of hydroxyethylene dipeptide-based β - secretase inhibitors ;

该文对β-分泌酶抑制剂的研究进展进行了综述。

The progress in the search of β - secretase inhibitors is reviewed in this article .

随后大量研究证明抑制γ-分泌酶是一个理想的药物发现靶点。

Inhibition of γ - secretase has proven to be a better target for drug discovery .

利用Gal4/VP16-UAS和双荧光素酶报告基因系统检测γ-分泌酶活性

Applying Gal4 / VP16-UAS and Dual-Luciferase reporter gene system to detecting the activity of γ - secretase

与Aβ相关的分泌酶及其在药物设计中的意义

Advances in A β - Related Secretases and Drug Design in the Therapy of Alzheimer 's Disease

慢性低氧低糖培养影响新生大鼠海马神经元α-分泌酶的实验研究

An experimental study of the effect on α - secretase of rat hippocampal neurons after chronic hypoxic and hypoglycemic culture

结论成功构建了β分泌酶抑制剂筛选模型并用于中草药提取物活性筛选。

Conclusion A screen assay of β - secretase inhibitors was successfully constructed and can be used to screen natural products .

这个结果暗示，γ分泌酶就像β分泌酶一样，也含有催化蛋白切割反应所必需的一对天冬胺酸。

This result suggested that gamma-secretase , like beta-secretase , contains a pair of aspartic acids essential for catalyzing the protein-cutting reaction .