ArticleScientific reports2017
New insights into the intracellular distribution pattern of cationic amphiphilic drugs.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 32 citations in OpenAlex.
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- Drug-induced phospholipidosis of the kidney suspected to be caused by atomoxetine.Journal of pathology and translational medicine · 2026Article
- A cationic amphiphilic drug synergizes with strobilurin fungicides to control fungal-borne plant diseases.Cell chemical biology · 2025Article
- The Antidepressant Drug Amitriptyline Affects Human SH-SY5Y Neuroblastoma Cell Proliferation and Modulates Autophagy.International journal of molecular sciences · 2024Article
- Stratifying macrophages based on their infectious burden identifies novel host targets for intervention during Crohn's disease associated adherent-invasiveMicrobiology (Reading, England) · 2024Article
- Endosomal Escape of Bioactives Deployed via Nanocarriers: Insights Into the Design of Polymeric Micelles.Pharmaceutical research · 2022Review
- Defending Antiviral Cationic Amphiphilic Drugs That May Cause Drug-Induced Phospholipidosis.Journal of chemical information and modeling · 2021Article
- The Anti-inflammatory Effect of the Tricyclic Antidepressant Clomipramine and Its High Penetration in the Brain Might Be Useful to Prevent the Psychiatric Consequences of SARS-CoV-2 Infection.Frontiers in pharmacology · 2021Article
- Psychotropic Drugs Show Anticancer Activity by Disrupting Mitochondrial and Lysosomal Function.Frontiers in oncology · 2020Article
- Repurposing Cationic Amphiphilic Drugs and Derivatives to Engage Lysosomal Cell Death in Cancer Treatment.Frontiers in oncology · 2020Review
- Integrating yeast chemical genomics and mammalian cell pathway analysis.Acta pharmacologica Sinica · 2019Article
- Dual lysosomal-mitochondrial targeting by antihistamines to eradicate leukaemic cells.EBioMedicine · 2019Article
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- Review
Corrections and comments
- Erratum issued
Authors and funding
13 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cationic amphiphilic drugs (CADs) comprise a wide variety of different substance classes such as antidepressants, antipsychotics, and antiarrhythmics. It is well recognized that CADs accumulate in certain intracellular compartments leading to specific morphological changes of cells. So far, no adequate technique exists allowing for ultrastructural analysis of CAD in intact cells. Azidobupramine, a recently described multifunctional antidepressant analogue, allows for the first time to perform high-resolution studies of CADs on distribution pattern and morphological changes in intact cells. We showed here that the intracellular distribution pattern of azidobupramine strongly depends on drug concentration and exposure time. The mitochondrial compartment (mDsRed) and the late endo-lysosomal compartment (CD63-GFP) were the preferred localization sites at low to intermediate concentrations (i.e. 1 μM, 5 μM). In contrast, the autophagosomal compartment (LC3-GFP) can only be reached at high concentrations (10 μM) and long exposure times (72 hrs). At the morphological level, LC3-clustering became only prominent at high concentrations (10 μM), while changes in CD63 pattern already occurred at intermediate concentrations (5 μM). To our knowledge, this is the first study that establishes a link between intracellular CAD distribution pattern and morphological changes. Therewith, our results allow for gaining deeper understanding of intracellular effects of CADs.
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