知道抑制剂的特异性取决于什么很有好处。

IF 13.3 1区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL
Aoife Murray, Ana Muñiz-García, Ivan Alić, Dean Nižetić
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引用次数: 0

摘要

淀粉样β肽(Aβ)的产生、聚集和清除是阿尔茨海默病(AD)最初发病机制的重要过程。迄今为止,抑制β位点淀粉样前体蛋白(APP)裂解酶(BACE1)(负责产生Aβ的两种关键蛋白酶之一)作为治疗阿尔茨海默病的方法还没有成功的药物。BACE1 及其同源物 BACE2 经常被同一种抑制剂所抑制。一些遗传和脑器官模型研究表明,BACE2具有剂量依赖性的AD抑制活性,这使得对其进行不必要的抑制可能会对AD治疗产生反作用。由于缺乏针对 BACE2 分裂的特异性药效学标记物,迄今为止还无法监测 BACE2 意外交叉抑制的体内效应。在本期的 JCI 杂志上,Stefan F. Lichtenthaler 领导的研究将可溶性血管内皮生长因子受体 3 (sVEGFR3) 鉴定为 BACE2 活性的药效学血浆标志物,而 BACE1 并不具有这种活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
It's good to know what to BACE the specificity of your inhibitors on.

Production, aggregation, and clearance of the amyloid β peptide (Aβ) are important processes governing the initial pathogenesis of Alzheimer's disease (AD). Inhibition of β-site amyloid precursor protein (APP) cleaving enzyme (BACE1) (one of two key proteases responsible for Aβ production) as an AD-therapeutic approach so far has failed to yield a successful drug. BACE1 and its homologue BACE2 are frequently inhibited by the same inhibitors. Several genetic and cerebral organoid modeling studies suggest that BACE2 has dose-dependent AD-suppressing activity, which makes its unwanted inhibition potentially counterproductive for AD treatment. The in vivo effects of an unwanted cross inhibition of BACE2 have so far been impossible to monitor because of the lack of an easily accessible pharmacodynamic marker specific for BACE2 cleavage. In this issue of the JCI, work led by Stefan F. Lichtenthaler identifies soluble VEGFR3 (sVEGFR3) as a pharmacodynamic plasma marker for BACE2 activity not shared with BACE1.

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来源期刊
Journal of Clinical Investigation
Journal of Clinical Investigation 医学-医学:研究与实验
CiteScore
24.50
自引率
1.30%
发文量
1034
审稿时长
2 months
期刊介绍: The Journal of Clinical Investigation, established in 1924 by the ASCI, is a prestigious publication that focuses on breakthroughs in basic and clinical biomedical science, with the goal of advancing the field of medicine. With an impressive Impact Factor of 15.9 in 2022, it is recognized as one of the leading journals in the "Medicine, Research & Experimental" category of the Web of Science. The journal attracts a diverse readership from various medical disciplines and sectors. It publishes a wide range of research articles encompassing all biomedical specialties, including Autoimmunity, Gastroenterology, Immunology, Metabolism, Nephrology, Neuroscience, Oncology, Pulmonology, Vascular Biology, and many others. The Editorial Board consists of esteemed academic editors who possess extensive expertise in their respective fields. They are actively involved in research, ensuring the journal's high standards of publication and scientific rigor.
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