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BACE-1信息

英文名称:Beta-secretase 1
中文名称:β-分泌酶-1
靶点别称:Beta-site amyloid precursor protein cleaving enzyme 1,KIAA1149,Asp 2,ASP2,Aspartyl protease 2,BACE,BACE1,Beta-Secretase 1,Membrane-Associated Aspartic Protease 2,Beta-Site APP-Cleaving Enzyme,Memapsin-2,Transmembrane Aspartic Proteinase Asp2,Beta-Site APP-Cleaving Enzyme 1,APP Beta-Secretase,EC 3.4.23.46,HSPC104,EC 3.4.23,Beta-Site APP Cleaving Enzyme 1,Beta-Site Amyloid Beta A4 Precursor Protein-Cleaving Enzyme,Beta-Secretase 1 Precursor Variant 1,EC:3.4.23.46
上市药物数量:0
临床药物数量:5
最高研发阶段:临床三期

BACE-1 分子别名

BACE1,ASP2,BACE,FLJ90568,HSPC104,KIAA1149,Memapsin-2

BACE-1 分子背景

Beta-secretase 1 (BACE1) is also known as beta-site APP cleaving enzyme 1 (beta-site amyloid precursor protein cleaving enzyme 1), memapsin-2 (membrane-associated aspartic protease 2), and aspartyl protease 2 (ASP2), β-Secretase , and is a member of the peptidase A1 protein family, BACE1 is a type I  integral membrane glycoprotein and aspartic protease that is found mainly in the Golgi. BACE1 is an aspartic-acid protease important in the pathogenesis of Alzheimer's disease, and in the formation of myelin sheaths in peripheral nerve cells. The transmembrane protein contains two active site aspartate residues in its extracellular protein domain and may function as a dimer. This protease is responsible for the proteolytic processing of the amyloid precursor protein (APP). Generation of the 40 or 42 amino acid-long amyloid-β peptides that aggregate in the brain of Alzheimer's patients requires two sequential cleavages of the APP. Extracellular cleavage of APP by BACE creates a soluble extracellular fragment and a cell membrane-bound fragment referred to as C99. The elevation of BACE1 levels can be induced by amyloid plaques surrounding neurons at early stages of pathology before neuron death occurs, and may drive a positive-feedback loop in AD.

BACE-1 前沿进展

BACE-1临床药物信息

英文名称 研发代码 研发阶段 公司 适应症 临床试验
Elenbecestat E-2609; [14C]E2609 临床三期 卫材株式会社 阿尔茨海默病 详情
Lanabecestat AZD-3293; LY-3314814 临床三期 阿斯利康制药有限公司 肾功能不全, 肝功能衰退, 阿尔茨海默病 详情
LY-3202626 LY-3202626 临床二期 礼来制药 阿尔茨海默病 详情
TAK-070 TAK-070 临床一期 武田药品工业株式会社 阿尔茨海默病 详情
Umibecestat AMG-520; CNP-520 临床三期 诺华制药 阿尔茨海默病 详情

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