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Literature DB >> 31307979

Repurposing Quinacrine against Ebola Virus Infection In Vivo.

Thomas R Lane¹, Jason E Comer^2,3,4, Alexander N Freiberg^4,5, Peter B Madrid⁶, Sean Ekins⁷.

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) in vitro 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.

Entities: Chemical Disease Species

Keywords: Ebola virus; Ebola virus disease; antiviral; quinacrine

Mesh：

Substances：

Year: 2019 PMID： 31307979 PMCID： PMC6709481 DOI： 10.1128/AAC.01142-19

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

30 in total

1. An evaluation of the in vitro metabolism data for predicting the clearance and drug-drug interaction potential of CYP2C9 substrates.

Authors: Tommy B Andersson; Eva Bredberg; Hans Ericsson; Helena Sjöberg
Journal: Drug Metab Dispos Date: 2004-07 Impact factor: 3.922

2. Implementation of an ADME enabling selection and visualization tool for drug discovery.

Authors: Chad L Stoner; Eric Gifford; Charles Stankovic; Christopher S Lepsy; Joanne Brodfuehrer; J V N Vara Prasad; Narayanan Surendran
Journal: J Pharm Sci Date: 2004-05 Impact factor: 3.534

3. Vaccinia virus entry into cells via a low-pH-dependent endosomal pathway.

Authors: Alan C Townsley; Andrea S Weisberg; Timothy R Wagenaar; Bernard Moss
Journal: J Virol Date: 2006-09 Impact factor: 5.103

4. Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection.

Authors: Sean Ekins; Mary A Lingerfelt; Jason E Comer; Alexander N Freiberg; Jon C Mirsalis; Kathleen O'Loughlin; Anush Harutyunyan; Claire McFarlane; Carol E Green; Peter B Madrid
Journal: Antimicrob Agents Chemother Date: 2018-01-25 Impact factor: 5.191

5. Antiviral activities of selected antimalarials against dengue virus type 2 and Zika virus.

Authors: Anuradha Balasubramanian; Tadahisa Teramoto; Amol A Kulkarni; Apurba K Bhattacharjee; Radhakrishnan Padmanabhan
Journal: Antiviral Res Date: 2016-11-23 Impact factor: 5.970

Review 6. ZIKA virus entry mechanisms in human cells.

Authors: Almerinda Agrelli; Ronald Rodrigues de Moura; Sergio Crovella; Lucas André Cavalcanti Brandão
Journal: Infect Genet Evol Date: 2019-01-15 Impact factor: 3.342

7. Chloroquine transport via the malaria parasite's chloroquine resistance transporter.

Authors: Rowena E Martin; Rosa V Marchetti; Anna I Cowan; Susan M Howitt; Stefan Bröer; Kiaran Kirk
Journal: Science Date: 2009-09-25 Impact factor: 47.728

Review 8. A bibliometric review of drug repurposing.

Authors: Nancy C Baker; Sean Ekins; Antony J Williams; Alexander Tropsha
Journal: Drug Discov Today Date: 2018-01-09 Impact factor: 7.851

Review 9. A simple practice guide for dose conversion between animals and human.

Authors: Anroop B Nair; Shery Jacob
Journal: J Basic Clin Pharm Date: 2016-03

10. Machine learning models identify molecules active against the Ebola virus in vitro.

Authors: Sean Ekins; Joel S Freundlich; Alex M Clark; Manu Anantpadma; Robert A Davey; Peter Madrid
Journal: F1000Res Date: 2015-10-20

17 in total

Review 1. Déjà vu: Stimulating open drug discovery for SARS-CoV-2.

Authors: Sean Ekins; Melina Mottin; Paulo R P S Ramos; Bruna K P Sousa; Bruno Junior Neves; Daniel H Foil; Kimberley M Zorn; Rodolpho C Braga; Megan Coffee; Christopher Southan; Ana C Puhl; Carolina Horta Andrade
Journal: Drug Discov Today Date: 2020-04-19 Impact factor: 7.851

2. Pyronaridine tetraphosphate efficacy against Ebola virus infection in guinea pig.

Authors: Thomas R Lane; Christopher Massey; Jason E Comer; Alexander N Freiberg; Huanying Zhou; Julie Dyall; Michael R Holbrook; Manu Anantpadma; Robert A Davey; Peter B Madrid; Sean Ekins
Journal: Antiviral Res Date: 2020-07-16 Impact factor: 5.970

3. Defending Antiviral Cationic Amphiphilic Drugs That May Cause Drug-Induced Phospholipidosis.

Authors: Thomas R Lane; Sean Ekins
Journal: J Chem Inf Model Date: 2021-09-13 Impact factor: 6.162

Review 4. Knowledge-based approaches to drug discovery for rare diseases.

Authors: Vinicius M Alves; Daniel Korn; Vera Pervitsky; Andrew Thieme; Stephen J Capuzzi; Nancy Baker; Rada Chirkova; Sean Ekins; Eugene N Muratov; Anthony Hickey; Alexander Tropsha
Journal: Drug Discov Today Date: 2021-10-27 Impact factor: 8.369

5. Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein.

Authors: Thomas R Lane; Sean Ekins
Journal: ACS Med Chem Lett Date: 2020-07-23 Impact factor: 4.345

6. Quantum Machine Learning Algorithms for Drug Discovery Applications.

Authors: Kushal Batra; Kimberley M Zorn; Daniel H Foil; Eni Minerali; Victor O Gawriljuk; Thomas R Lane; Sean Ekins
Journal: J Chem Inf Model Date: 2021-05-25 Impact factor: 6.162

7. Repurposing the Ebola and Marburg Virus Inhibitors Tilorone, Quinacrine and Pyronaridine: In vitro Activity Against SARS-CoV-2 and Potential Mechanisms.

Authors: Ana C Puhl; Ethan James Fritch; Thomas R Lane; Longping V Tse; Boyd L Yount; Carol Queiroz Sacramento; Tatyana Almeida Tavella; Fabio Trindade Maranhão Costa; Stuart Weston; James Logue; Matthew Frieman; Lakshmanane Premkumar; Kenneth H Pearce; Brett L Hurst; Carolina Horta Andrade; James A Levi; Nicole J Johnson; Samantha C Kisthardt; Frank Scholle; Thiago Moreno L Souza; Nathaniel John Moorman; Ralph S Baric; Peter Madrid; Sean Ekins
Journal: bioRxiv Date: 2020-12-02