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了解针对抑制剂特异性的 BACE 很重要。

It's good to know what to BACE the specificity of your inhibitors on.

机构信息

The Blizard Institute, Faculty of Medicine and Dentistry, Queen Mary University of London, London, United Kingdom.

Department of Anatomy, Histology and Embryology, Faculty of Veterinary Medicine, University of Zagreb, Zagreb, Croatia.

出版信息

J Clin Invest. 2024 Aug 15;134(16):e183677. doi: 10.1172/JCI183677.

Abstract

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.

摘要

淀粉样 β 肽 (Aβ) 的产生、聚集和清除是控制阿尔茨海默病 (AD) 初始发病机制的重要过程。迄今为止,抑制 β 位淀粉样前体蛋白 (APP) 裂解酶 (BACE1)(负责 Aβ 产生的两种关键蛋白酶之一)作为 AD 治疗方法并未产生成功的药物。BACE1 和其同源物 BACE2 经常被相同的抑制剂抑制。几项遗传和脑类器官建模研究表明,BACE2 具有剂量依赖性的 AD 抑制活性,这使得其不受欢迎的抑制对 AD 治疗可能适得其反。由于缺乏针对 BACE2 裂解的易于获得的特异性药效学标志物,迄今为止,BACE2 不受控制的交叉抑制的体内效应一直无法监测。在本期 JCI 中,Stefan F. Lichtenthaler 领导的工作将可溶性 VEGFR3 (sVEGFR3) 确定为 BACE2 活性的药效学血浆标志物,与 BACE1 没有共享。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/297b/11324289/6e8d06bc3896/jci-134-183677-g109.jpg

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