ArticleAntimicrobial agents and chemotherapy2020
Filovirus Antiviral Activity of Cationic Amphiphilic Drugs Is Associated with Lipophilicity and Ability To Induce Phospholipidosis.
Article in Antimicrobial agents and chemotherapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Guardians at the Gate: Optimization of Small Molecule Entry Inhibitors of Ebola and Marburg Viruses.Journal of medicinal chemistry · 2025Article
- Evaluation of potency and metabolic stability of diphyllin-derived Vacuolar-ATPase inhibitors.European journal of medicinal chemistry · 2024Article
- AMALPHI: A Machine Learning Platform for Predicting Drug-Induced PhospholIpidosis.Molecular pharmaceutics · 2024Article
- Sub-cellular sequestration of alkaline drugs in lysosomes: new insights for pharmaceutical development of lysosomal fluid.Research in pharmaceutical sciences · 2023Article
- Identification of potent inhibitors of SARS-CoV-2 infection by combined pharmacological evaluation and cellular network prioritization.iScience · 2022Article
- Sites of vulnerability in HCV E1E2 identified by comprehensive functional screening.Cell reports · 2022Article
- Evaluation of Phenol-Substituted Diphyllin Derivatives as Selective Antagonists for Ebola Virus Entry.ACS infectious diseases · 2022Article
- Implicitly perturbed Hamiltonian as a class of versatile and general-purpose molecular representations for machine learning.Nature communications · 2022Article
- Spiers Memorial Lecture: Analysis andFaraday discussions · 2021Article
- Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2.Science (New York, N.Y.) · 2021Article
- Interdependent Impact of Lipoprotein Receptors and Lipid-Lowering Drugs on HCV Infectivity.Cells · 2021Article
- Phospholipidosis is a shared mechanism underlying thebioRxiv : the preprint server for biology · 2021Article
- Nuisance compounds in cellular assays.Cell chemical biology · 2021Review
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Several cationic amphiphilic drugs (CADs) have been found to inhibit cell entry of filoviruses and other enveloped viruses. Structurally unrelated CADs may have antiviral activity, yet the underlying common mechanism and structure-activity relationship are incompletely understood. We aimed to understand how widespread antiviral activity is among CADs and which structural and physico-chemical properties are linked to entry inhibition. We measured inhibition of Marburg virus pseudoparticle (MARVpp) cell entry by 45 heterogeneous and mostly FDA-approved CADs and cytotoxicity in EA.hy926 cells. We analyzed correlation of antiviral activity with four chemical properties: pKa, hydrophobicity (octanol/water partitioning coefficient; ClogP), molecular weight, and distance between the basic group and hydrophobic ring structures. Additionally, we quantified drug-induced phospholipidosis (DIPL) of a CAD subset by flow cytometry. Structurally similar compounds (derivatives) and those with similar chemical properties but unrelated structures (analogues) to those of strong inhibitors were obtained by two
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.