ArticleMolecular cancer2013
Inhibition of clathrin by pitstop 2 activates the spindle assembly checkpoint and induces cell death in dividing HeLa cancer cells.
Article in Molecular cancer, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 51 citations in OpenAlex.
- Functional Specialization of Clathrin-Independent Endocytic Routes: Mechanisms and Cellular Roles.Traffic (Copenhagen, Denmark) · 2026Review
- Polymeric mesoscale nanoparticles exhibit dynamin- and macropinocytosis-dependent endocytosis.Nanomedicine : nanotechnology, biology, and medicine · 2026Article
- Endocytosis of PEGylated polymeric mesoscale nanoparticles is dynamin- and macropinocytosis-dependent.bioRxiv : the preprint server for biology · 2026Article
- Spatiotemporal Regulation of Ligand Trafficking and TLR9 Activation by PIEZO1 in Human Plasmacytoid Dendritic Cells.Research (Washington, D.C.) · 2026Article
- Clathrin mediated endocytosis targeting chimera for targeted membrane proteins degradation and enhance CAR-T cell anti-tumor therapy.Theranostics · 2026Article
- Targeting clathrin-mediated endocytosis: recent advances in inhibitor development, mechanistic insights, and therapeutic prospects.RSC medicinal chemistry · 2025Review
- Inhibition of the Clathrin Terminal Domain-Amphiphysin Protein-Protein Interaction. Probing the Pitstop 2 Aromatic Moiety.ChemMedChem · 2025Article
- Article
- Targeting endocytosis to sensitize cancer cells to programmed cell death.Biochemical Society transactions · 2024Review
- The AP-2 complex interacts with γ-TuRC and regulates the proliferative capacity of neural progenitors.Life science alliance · 2024Article
- Biomechanics-mediated endocytosis in atherosclerosis.Frontiers in cardiovascular medicine · 2024Review
- Human Immunodeficiency Virus 1 Preferentially Fuses with pH-Neutral Endocytic Vesicles in Cell Lines and Human Primary CD4+ T-Cells.ACS nano · 2023Article
- Pitstop-2 and its novel derivative RVD-127 disrupt global cell dynamics and nuclear pores integrity by direct interaction with small GTPases.Bioengineering & translational medicine · 2023Article
- Opposite changes in the expression of clathrin and caveolin-1 in normal and cancerous human prostate tissue: putative clathrin-mediated recycling of EGFR.Histochemistry and cell biology · 2023Article
- Mechanistic-Based Classification of Endocytosis-Related Inhibitors: Does It Aid in Assigning Drugs against SARS-CoV-2?Viruses · 2023Review
- Human Adenovirus Type 26 Infection Mediated by αvβ3 Integrin Is Caveolin-1-Dependent.Microbiology spectrum · 2022Article
- The uptake of metal-organic frameworks: a journey into the cell.Chemical Society reviews · 2022Review
- Exploration and insights into the cellular internalization and intracellular fate of amphiphilic polymeric nanocarriers.Acta pharmaceutica Sinica. B · 2021Review
- Role of Clathrin and Dynamin in Clathrin Mediated Endocytosis/Synaptic Vesicle Recycling and Implications in Neurological Diseases.Frontiers in cellular neuroscience · 2021Review
- Wbox2: A clathrin terminal domain-derived peptide inhibitor of clathrin-mediated endocytosis.The Journal of cell biology · 2020Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundDuring metaphase clathrin stabilises the mitotic spindle kinetochore (K)-fibres. Many anti-mitotic compounds target microtubule dynamics. Pitstop 2™ is the first small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis. We investigated its effects on a second function for clathrin in mitosis.
resultsPitstop 2 did not impair clathrin recruitment to the spindle but disrupted its function once stationed there. Pitstop 2 trapped HeLa cells in metaphase through loss of mitotic spindle integrity and activation of the spindle assembly checkpoint, phenocopying clathrin depletion and aurora A kinase inhibition.
conclusionsPitstop 2 is therefore a new tool for investigating clathrin spindle dynamics. Pitstop 2 reduced viability in dividing HeLa cells, without affecting dividing non-cancerous NIH3T3 cells, suggesting that clathrin is a possible novel anti-mitotic drug target.
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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.