ArticleBritish journal of pharmacology2018
Identification of novel macropinocytosis inhibitors using a rational screen of Food and Drug Administration-approved drugs.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 88 papers.
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Who cites it
88 citing papers in PubMed, 135 citations in OpenAlex.
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- Functional Specialization of Clathrin-Independent Endocytic Routes: Mechanisms and Cellular Roles.Traffic (Copenhagen, Denmark) · 2026Review
- Dual targeting of SLC6A14 and autophagy/macropinocytosis enhances therapeutic efficacy in pancreatic ductal adenocarcinoma.The Biochemical journal · 2026Article
- Beyond the scaffold: extracellular matrix uptake in breast cancer.Biochemical Society transactions · 2026Review
- Mechanistic Insights into Redox-Dependent Macropinocytosis in Primary Human Neutrophils.Antioxidants (Basel, Switzerland) · 2026Article
- Macropinocytosis inhibition attenuates profibrotic responses in lung fibroblasts and pulmonary fibrosis models.The Journal of clinical investigation · 2026Article
- CORE: Cholesterol Altered Lipid Nanoparticles for Splenic Expression of mRNA Payloads.Advanced healthcare materials · 2026Article
- A Physiological Microfluidic Blood-Brain-Barrier Model for In Vitro Study of Nanoparticle Trafficking and Accumulation.Advanced healthcare materials · 2026Article
- Syndecan-1-targeted therapeutic antibody impairs macropinocytosis and elicits antitumor immunity in pancreatic cancer.Cell reports. Medicine · 2026Article
- Dose Delays and Treatment Interruptions Secondary to Ocular Toxicity From BCMA-Directed Antibody Drug Conjugate Therapy in Relapsed Multiple Myeloma.Clinical lymphoma, myeloma & leukemia · 2026Article
- ATP increases murine neuroblastoma cell size through a PANX1- and macropinocytosis-dependent mechanism.Biology open · 2025Article
- Polyethyleneimine-modifiedMaterials today. Bio · 2025Article
- RNA activation ofMolecular therapy. Nucleic acids · 2025Article
- A physiological microfluidic blood-brain-barrier model for in vitro study of nanoparticle trafficking and accumulation.bioRxiv : the preprint server for biology · 2025Article
- Glutathione hybrid poly (beta-amino ester)-plasmid nanoparticles for enhancing gene delivery and biosafety.Journal of advanced research · 2025Article
- Immunomodulatory Nanoparticles Induce Autophagy in Macrophages and ReduceACS infectious diseases · 2025Article
- Differences in Phage Recognition and Immunogenicity Contribute to Divergent Human Immune Responses to Escherichia coli and Klebsiella pneumoniae Phages.European journal of immunology · 2025Article
- Harnessing macrophage-drug conjugates for allogeneic cell-based therapy of solid tumors via the TRAIN mechanism.Nature communications · 2025Article
28 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
background and purposeMacropinocytosis is involved in many pathologies, including cardiovascular disorders, cancer, allergic diseases, viral and bacterial infections. Unfortunately, the currently available pharmacological inhibitors of macropinocytosis interrupt other endocytic processes and have non-specific endocytosis-independent effects. Here we have sought to identify new, clinically relevant inhibitors of macropinocytosis, using an FDA-approved drug library. EXPERIMENTAL APPROACH: In the present study, 640 FDA-approved compounds were tested for their ability to inhibit macropinocytosis. A series of secondary assays were performed to confirm inhibitory activity, determine IC KEY
resultsThe primary screen identified 14 compounds that at ~10 μM concentration inhibit >95% of macropinocytotic solute internalization. Three compounds - imipramine, phenoxybenzamine and vinblastine - potently inhibited (IC CONCLUSIONS AND IMPLICATIONS: Our results identify imipramine as a new pharmacological tool to study macropinocytosis in cellular and biological systems. This study also suggests that imipramine could be a good candidate for repurposing as a therapeutic agent in pathological processes involving macropinocytosis.
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Registered trials
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.