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本文引用的文献

1
Ebola Virus Bayesian Machine Learning Models Enable New in Vitro Leads.埃博拉病毒贝叶斯机器学习模型带来新的体外研究线索。
ACS Omega. 2019 Jan 31;4(1):2353-2361. doi: 10.1021/acsomega.8b02948. Epub 2019 Jan 30.
2
ZIKA virus entry mechanisms in human cells.寨卡病毒进入人体细胞的机制。
Infect Genet Evol. 2019 Apr;69:22-29. doi: 10.1016/j.meegid.2019.01.018. Epub 2019 Jan 15.
3
High Throughput and Computational Repurposing for Neglected Diseases.高通量筛选与计算药物重用以治疗被忽视疾病。
Pharm Res. 2018 Dec 17;36(2):27. doi: 10.1007/s11095-018-2558-3.
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Safety, pharmacokinetics, and immunogenicity of a co-formulated cocktail of three human monoclonal antibodies targeting Ebola virus glycoprotein in healthy adults: a randomised, first-in-human phase 1 study.在健康成年人中,三种靶向埃博拉病毒糖蛋白的人源单克隆抗体鸡尾酒的安全性、药代动力学和免疫原性:一项随机、首次人体的 1 期研究。
Lancet Infect Dis. 2018 Aug;18(8):884-893. doi: 10.1016/S1473-3099(18)30397-9. Epub 2018 Jun 18.
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A bibliometric review of drug repurposing.药物重定位的文献计量学研究
Drug Discov Today. 2018 Mar;23(3):661-672. doi: 10.1016/j.drudis.2018.01.018. Epub 2018 Jan 9.
6
Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection.盐酸替洛隆对埃博拉病毒感染的疗效。
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.01711-17. Print 2018 Feb.
7
Antiviral activities of selected antimalarials against dengue virus type 2 and Zika virus.某些抗疟药对登革2型病毒和寨卡病毒的抗病毒活性。
Antiviral Res. 2017 Jan;137:141-150. doi: 10.1016/j.antiviral.2016.11.015. Epub 2016 Nov 23.
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A simple practice guide for dose conversion between animals and human.动物与人之间剂量转换的简易实践指南。
J Basic Clin Pharm. 2016 Mar;7(2):27-31. doi: 10.4103/0976-0105.177703.
9
Chasing Ebola through the Endosomal Labyrinth.在内体迷宫中追踪埃博拉病毒
mBio. 2016 Mar 22;7(2):e00346. doi: 10.1128/mBio.00346-16.
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Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.小分子GS-5734对恒河猴体内埃博拉病毒的治疗效果。
Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2.

抗埃博拉病毒感染的奎纳克林再利用。

Repurposing Quinacrine against Ebola Virus Infection .

机构信息

Collaborations Pharmaceuticals, Inc., Raleigh, North Carolina, USA.

Department of Microbiology and Immunology, University of Texas Medical Branch, Galveston, Texas, USA.

出版信息

Antimicrob Agents Chemother. 2019 Aug 23;63(9). doi: 10.1128/AAC.01142-19. Print 2019 Sep.

DOI:10.1128/AAC.01142-19
PMID:31307979
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6709481/
Abstract

Quinacrine hydrochloride is a small-molecule, orally bioavailable drug that has been used clinically as an antimalarial and for many other applications. A machine learning model trained on Ebola virus (EBOV) screening data identified quinacrine as a potent (nanomolar) inhibitor. In the current study, quinacrine 25 mg/kg was shown to protect 70% of mice (statistically significant) from a lethal challenge with mouse-adapted EBOV with once-daily intraperitoneal dosing for 8 days.

摘要

盐酸奎宁是一种小分子、口服生物利用的药物,临床上已被用作抗疟药和许多其他用途。一个基于埃博拉病毒 (EBOV) 筛选数据训练的机器学习模型将奎宁鉴定为一种有效的(纳摩尔级)抑制剂。在目前的研究中,每天一次腹腔内给药 8 天,25mg/kg 的奎宁可保护 70%的小鼠(具有统计学意义)免受致死性的适应小鼠的埃博拉病毒的攻击。