• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

β-分泌酶1（BACE1）抑制剂的研发与结构修饰

Development and Structural Modification of BACE1 Inhibitors.

作者信息

Gu Ting, Wu Wen-Yu, Dong Ze-Xi, Yu Shao-Peng, Sun Ying, Zhong Yue, Lu Yu-Ting, Li Nian-Guang

机构信息

Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, Jiangsu, China.

出版信息

Molecules. 2016 Dec 22;22(1):4. doi: 10.3390/molecules22010004.

DOI:10.3390/molecules22010004
PMID:28025519
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6155942/
Abstract

Alzheimer's disease (AD) is a progressive neurodegenerative disorder which usually occurs in the elderly. The accumulation of β-amyloid and the formation of neurofibrillary tangles are considered as the main pathogenies of AD. Research suggests that β-secretase 1 (BACE1) plays an important role in the formation of β-amyloid. Discovery of new BACE1 inhibitors has become a significant method to slow down the progression of AD or even cure this kind of disease. This review summarizes the different types and the structural modification of these new BACE1 inhibitors.

摘要

阿尔茨海默病（AD）是一种通常发生在老年人身上的进行性神经退行性疾病。β-淀粉样蛋白的积累和神经纤维缠结的形成被认为是AD的主要发病机制。研究表明，β-分泌酶1（BACE1）在β-淀粉样蛋白的形成中起重要作用。发现新的BACE1抑制剂已成为减缓AD进展甚至治愈这种疾病的重要方法。本文综述了这些新型BACE1抑制剂的不同类型及其结构修饰。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/86ca371198c1/molecules-22-00004-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/b16734a178d0/molecules-22-00004-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/095b04738e91/molecules-22-00004-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/c4696ef829b6/molecules-22-00004-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/a3e4257505d5/molecules-22-00004-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/ecac323dd330/molecules-22-00004-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/13059984c864/molecules-22-00004-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/5ef1622ef25d/molecules-22-00004-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/bcf317352783/molecules-22-00004-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/40ca9834b04b/molecules-22-00004-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/fca9cb9812c1/molecules-22-00004-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/86ca371198c1/molecules-22-00004-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/b16734a178d0/molecules-22-00004-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/095b04738e91/molecules-22-00004-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/c4696ef829b6/molecules-22-00004-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/a3e4257505d5/molecules-22-00004-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/ecac323dd330/molecules-22-00004-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/13059984c864/molecules-22-00004-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/5ef1622ef25d/molecules-22-00004-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/bcf317352783/molecules-22-00004-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/40ca9834b04b/molecules-22-00004-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/fca9cb9812c1/molecules-22-00004-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0370/6155942/86ca371198c1/molecules-22-00004-g011.jpg

相似文献

1
Development and Structural Modification of BACE1 Inhibitors.β-分泌酶1（BACE1）抑制剂的研发与结构修饰
Molecules. 2016 Dec 22;22(1):4. doi: 10.3390/molecules22010004.
2
BACE1 in Alzheimer's disease.β 分泌酶 1 在阿尔茨海默病中的作用。
Clin Chim Acta. 2012 Dec 24;414:171-8. doi: 10.1016/j.cca.2012.08.013. Epub 2012 Aug 20.
3
A stereoselective approach to peptidomimetic BACE1 inhibitors.一种对映选择性的肽拟似 BACE1 抑制剂方法。
Eur J Med Chem. 2013;70:233-47. doi: 10.1016/j.ejmech.2013.09.056. Epub 2013 Oct 6.
4
Multifunctional iminochromene-2H-carboxamide derivatives containing different aminomethylene triazole with BACE1 inhibitory, neuroprotective and metal chelating properties targeting Alzheimer's disease.含不同氨基亚甲基三唑的多功能亚氨基苯并二氢吡喃-2H-甲酰胺衍生物，具有针对阿尔茨海默病的β-分泌酶1抑制、神经保护和金属螯合特性。
Eur J Med Chem. 2017 Dec 1;141:690-702. doi: 10.1016/j.ejmech.2017.09.057. Epub 2017 Sep 28.
5
Beta-secretase inhibitors in phase I and phase II clinical trials for Alzheimer's disease.β-分泌酶抑制剂在阿尔茨海默病的 I 期和 II 期临床试验中。
Expert Opin Investig Drugs. 2017 Oct;26(10):1131-1136. doi: 10.1080/13543784.2017.1369527. Epub 2017 Aug 23.
6
Curcumin Ameliorates Memory Decline via Inhibiting BACE1 Expression and β-Amyloid Pathology in 5×FAD Transgenic Mice.姜黄素通过抑制5×FAD转基因小鼠中β-分泌酶1（BACE1）的表达和β-淀粉样蛋白病理来改善记忆衰退。
Mol Neurobiol. 2017 Apr;54(3):1967-1977. doi: 10.1007/s12035-016-9802-9. Epub 2016 Feb 24.
7
Recent Studies on Design and Development of Drugs Against Alzheimer's Disease (AD) Based on Inhibition of BACE-1 and Other AD-causative Agents.近年来基于 BACE-1 抑制及其他 AD 致病因子的抗阿尔茨海默病药物的设计与开发研究。
Curr Top Med Chem. 2020;20(13):1195-1213. doi: 10.2174/1568026620666200416091623.
8
BACE1 Function and Inhibition: Implications of Intervention in the Amyloid Pathway of Alzheimer's Disease Pathology.BACE1 的功能及其抑制：阿尔茨海默病淀粉样病变途径干预的意义。
Molecules. 2017 Oct 13;22(10):1723. doi: 10.3390/molecules22101723.
9
From Kinase Inhibitors to Multitarget Ligands as Powerful Drug Leads for Alzheimer's Disease using Protein-Templated Synthesis.从激酶抑制剂到多靶点配体：基于蛋白质模板合成的阿尔茨海默病强效药物先导物
Angew Chem Int Ed Engl. 2021 Aug 23;60(35):19344-19354. doi: 10.1002/anie.202106295. Epub 2021 Jul 26.
10
Identification of a BACE1 Binding Peptide Candidate for the Prevention of Amyloid Beta in Alzheimer's Disease.鉴定一种用于预防阿尔茨海默病中β淀粉样蛋白的β分泌酶1结合肽候选物。
Cell Physiol Biochem. 2019;53(2):413-428. doi: 10.33594/000000147.

引用本文的文献

1
A molecular video-derived foundation model for scientific drug discovery.用于科学药物发现的基于分子视频的基础模型。
Nat Commun. 2024 Nov 8;15(1):9696. doi: 10.1038/s41467-024-53742-z.
2
Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates.黄酮类和查尔酮类骨架作为β-分泌酶1（BACE1）抑制剂的最新进展
Comb Chem High Throughput Screen. 2024;27(9):1243-1256. doi: 10.2174/1386207326666230731092409.
3
Ethnomedicinal Plants with Protective Effects against Beta-Amyloid Peptide (Aβ)1-42 Indicate Therapeutic Potential in a New In Vivo Model of Alzheimer's Disease.

本文引用的文献

1
Multi-target screening mines hesperidin as a multi-potent inhibitor: Implication in Alzheimer's disease therapeutics.多靶点筛选确定橙皮苷为一种多效抑制剂：对阿尔茨海默病治疗的启示。
Eur J Med Chem. 2016 Oct 4;121:810-822. doi: 10.1016/j.ejmech.2016.03.057. Epub 2016 Mar 29.
2
Exercise as a pro-cognitive, pro-neurogenic and anti-inflammatory intervention in transgenic mouse models of Alzheimer's disease.运动作为阿尔茨海默病转基因小鼠模型中的一种促进认知、促进神经发生和抗炎干预措施。
Ageing Res Rev. 2016 May;27:77-92. doi: 10.1016/j.arr.2016.03.007. Epub 2016 Mar 31.
3
MicroRNA-107 prevents amyloid-beta induced blood-brain barrier disruption and endothelial cell dysfunction by targeting Endophilin-1.
对β-淀粉样肽（Aβ）1-42具有保护作用的民族药用植物在阿尔茨海默病新体内模型中显示出治疗潜力。
Antioxidants (Basel). 2022 Sep 21;11(10):1865. doi: 10.3390/antiox11101865.
4
BACE1: A Key Regulator in Alzheimer's Disease Progression and Current Development of its Inhibitors.BACE1：阿尔茨海默病进展中的关键调节因子及其抑制剂的研究进展。
Curr Neuropharmacol. 2022;20(6):1174-1193. doi: 10.2174/1570159X19666211201094031.
5
Combining Virtual Screening Protocol and In Vitro Evaluation towards the Discovery of BACE1 Inhibitors.结合虚拟筛选方案和体外评估发现 BACE1 抑制剂。
Biomolecules. 2020 Apr 1;10(4):535. doi: 10.3390/biom10040535.
6
Reduction of Aβ Generation by Schisandrin B through Restraining Beta-Secretase 1 Transcription and Translation.五味子丙素通过抑制β-分泌酶 1 的转录和翻译减少 Aβ 的产生。
Med Sci Monit. 2018 Feb 28;24:1219-1224. doi: 10.12659/msm.905127.
7
Can brain impermeable BACE1 inhibitors serve as anti-CAA medicine?脑穿透性 BACE1 抑制剂能否作为抗脑动脉淀粉样血管病药物？
BMC Neurol. 2017 Aug 25;17(1):163. doi: 10.1186/s12883-017-0942-y.
8
C-C Carbocyclic-Fused Iminothiadiazine Dioxides as BACE Inhibitors, Their Compositions, and Their Use.作为β-分泌酶（BACE）抑制剂的C-C碳环稠合亚氨基噻二嗪二氧化物、其组合物及其用途
ACS Med Chem Lett. 2017 Jul 25;8(8):786-788. doi: 10.1021/acsmedchemlett.7b00268. eCollection 2017 Aug 10.
微小RNA-107通过靶向内吞蛋白-1来预防淀粉样β蛋白诱导的血脑屏障破坏和内皮细胞功能障碍。
Exp Cell Res. 2016 May 1;343(2):248-257. doi: 10.1016/j.yexcr.2016.03.026. Epub 2016 Mar 30.
4
Imbalanced cholesterol metabolism in Alzheimer's disease.阿尔茨海默病中的胆固醇代谢失衡。
Clin Chim Acta. 2016 May 1;456:107-114. doi: 10.1016/j.cca.2016.02.024. Epub 2016 Mar 2.
5
Nano-biosensors to detect beta-amyloid for Alzheimer's disease management.用于阿尔茨海默病管理中检测β-淀粉样蛋白的纳米生物传感器。
Biosens Bioelectron. 2016 Jun 15;80:273-287. doi: 10.1016/j.bios.2016.01.065. Epub 2016 Jan 28.
6
Kinetics and molecular docking studies of fucosterol and fucoxanthin, BACE1 inhibitors from brown algae Undaria pinnatifida and Ecklonia stolonifera.来自褐藻裙带菜和匍匐马尾藻的β-分泌酶1抑制剂岩藻甾醇和岩藻黄质的动力学及分子对接研究
Food Chem Toxicol. 2016 Mar;89:104-11. doi: 10.1016/j.fct.2016.01.014. Epub 2016 Jan 26.
7
Alzheimer's disease: An overview of amyloid beta dependent pathogenesis and its therapeutic implications along with in silico approaches emphasizing the role of natural products.阿尔茨海默病：淀粉样β蛋白依赖性发病机制概述及其治疗意义，以及强调天然产物作用的计算机模拟方法。
J Neurol Sci. 2016 Feb 15;361:256-71. doi: 10.1016/j.jns.2016.01.008. Epub 2016 Jan 8.
8
Application of BACE1 immobilized enzyme reactor for the characterization of multifunctional alkaloids from Corydalis cava (Fumariaceae) as Alzheimer's disease targets.BACE1固定化酶反应器在表征紫堇（罂粟科）中作为阿尔茨海默病靶点的多功能生物碱方面的应用。
Fitoterapia. 2016 Mar;109:241-7. doi: 10.1016/j.fitote.2016.01.008. Epub 2016 Jan 11.
9
D5 receptor agonist 027075 promotes cognitive function recovery and neurogenesis in a Aβ1-42-induced mouse model.D5受体激动剂027075在Aβ1-42诱导的小鼠模型中促进认知功能恢复和神经发生。
Neuropharmacology. 2016 Jun;105:72-83. doi: 10.1016/j.neuropharm.2016.01.008. Epub 2016 Jan 7.
10
BIIB042, a novel γ-secretase modulator, reduces amyloidogenic Aβ isoforms in primates and rodents and plaque pathology in a mouse model of Alzheimer's disease.BIIB042是一种新型γ-分泌酶调节剂，可减少灵长类动物和啮齿动物中淀粉样蛋白生成的Aβ异构体，并减轻阿尔茨海默病小鼠模型中的斑块病理。
Neuropharmacology. 2016 Apr;103:57-68. doi: 10.1016/j.neuropharm.2015.12.006. Epub 2015 Dec 12.