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.
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。
相似文献
1
Repurposing Quinacrine against Ebola Virus Infection .
Antimicrob Agents Chemother. 2019 Aug 23;63(9). doi: 10.1128/AAC.01142-19. Print 2019 Sep.
2
Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection.
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.01711-17. Print 2018 Feb.
3
Repurposing Pyramax®, quinacrine and tilorone as treatments for Ebola virus disease.
Antiviral Res. 2020 Oct;182:104908. doi: 10.1016/j.antiviral.2020.104908. Epub 2020 Aug 13.
4
Antiviral effect of ranpirnase against Ebola virus.
Antiviral Res. 2016 Aug;132:210-8. doi: 10.1016/j.antiviral.2016.06.009. Epub 2016 Jun 25.
5
Cholesterol-conjugated stapled peptides inhibit Ebola and Marburg viruses in vitro and in vivo.
Antiviral Res. 2019 Nov;171:104592. doi: 10.1016/j.antiviral.2019.104592. Epub 2019 Aug 29.
6
Repurposing the antimalarial pyronaridine tetraphosphate to protect against Ebola virus infection.
PLoS Negl Trop Dis. 2019 Nov 21;13(11):e0007890. doi: 10.1371/journal.pntd.0007890. eCollection 2019 Nov.
7
Prophylactic Efficacy of Quercetin 3-β-O-d-Glucoside against Ebola Virus Infection.
Antimicrob Agents Chemother. 2016 Aug 22;60(9):5182-8. doi: 10.1128/AAC.00307-16. Print 2016 Sep.
8
Pyronaridine tetraphosphate efficacy against Ebola virus infection in guinea pig.
Antiviral Res. 2020 Sep;181:104863. doi: 10.1016/j.antiviral.2020.104863. Epub 2020 Jul 16.
9
Assessing Antiviral Countermeasures Using Mouse Models of Ebolavirus Infection.
Methods Mol Biol. 2017;1628:273-282. doi: 10.1007/978-1-4939-7116-9_22.
10
Arbidol and Other Low-Molecular-Weight Drugs That Inhibit Lassa and Ebola Viruses.
J Virol. 2019 Apr 3;93(8). doi: 10.1128/JVI.02185-18. Print 2019 Apr 15.
引用本文的文献
1
Learning from COVID-19: How drug hunters can prepare for the next pandemic.
Drug Discov Today. 2023 Oct;28(10):103723. doi: 10.1016/j.drudis.2023.103723. Epub 2023 Jul 22.
2
Transporter Inhibition Profile for the Antivirals Tilorone, Quinacrine and Pyronaridine.
ACS Omega. 2023 Mar 24;8(13):12532-12537. doi: 10.1021/acsomega.3c00724. eCollection 2023 Apr 4.
3
Quinacrine-CASIN combination overcomes chemoresistance in human acute lymphoid leukemia.
Nat Commun. 2021 Nov 26;12(1):6936. doi: 10.1038/s41467-021-27300-w.
4
Knowledge-based approaches to drug discovery for rare diseases.
Drug Discov Today. 2022 Feb;27(2):490-502. doi: 10.1016/j.drudis.2021.10.014. Epub 2021 Oct 27.
5
Defending Antiviral Cationic Amphiphilic Drugs That May Cause Drug-Induced Phospholipidosis.
J Chem Inf Model. 2021 Sep 27;61(9):4125-4130. doi: 10.1021/acs.jcim.1c00903. Epub 2021 Sep 13.
6
Quinacrine, an Old Drug with Potentially usefull in the Treatment for COVID-19.
Arch Med Res. 2021 Nov;52(8):858-859. doi: 10.1016/j.arcmed.2021.06.002. Epub 2021 Jun 7.
7
Quinacrine directly dissociates amyloid plaques in the brain of 5XFAD transgenic mouse model of Alzheimer's disease.
Sci Rep. 2021 Jun 8;11(1):12043. doi: 10.1038/s41598-021-91563-y.
8
Quantum Machine Learning Algorithms for Drug Discovery Applications.
J Chem Inf Model. 2021 Jun 28;61(6):2641-2647. doi: 10.1021/acs.jcim.1c00166. Epub 2021 May 25.
9
Repurposing the Ebola and Marburg Virus Inhibitors Tilorone, Quinacrine, and Pyronaridine: Activity against SARS-CoV-2 and Potential Mechanisms.
ACS Omega. 2021 Mar 10;6(11):7454-7468. doi: 10.1021/acsomega.0c05996. eCollection 2021 Mar 23.
10
Quinacrine, an Antimalarial Drug with Strong Activity Inhibiting SARS-CoV-2 Viral Replication In Vitro.
Viruses. 2021 Jan 17;13(1):121. doi: 10.3390/v13010121.
本文引用的文献
1
Ebola Virus Bayesian Machine Learning Models Enable New in Vitro Leads.
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.
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.
Pharm Res. 2018 Dec 17;36(2):27. doi: 10.1007/s11095-018-2558-3.
4
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.
Lancet Infect Dis. 2018 Aug;18(8):884-893. doi: 10.1016/S1473-3099(18)30397-9. Epub 2018 Jun 18.
5
A bibliometric review of drug repurposing.
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.
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.
Antiviral Res. 2017 Jan;137:141-150. doi: 10.1016/j.antiviral.2016.11.015. Epub 2016 Nov 23.
8
A simple practice guide for dose conversion between animals and human.
J Basic Clin Pharm. 2016 Mar;7(2):27-31. doi: 10.4103/0976-0105.177703.
9
Chasing Ebola through the Endosomal Labyrinth.
mBio. 2016 Mar 22;7(2):e00346. doi: 10.1128/mBio.00346-16.
10
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.
Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2.
Zotero 插件