ArticleNature chemical biology2014
Unraveling the mechanism of cell death induced by chemical fibrils.
Article in Nature chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed.
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- Exploring Passive Permeability Profiles of Cyclic Heptapeptide Chemical Space Uncovers Bioactivity of Mortiamide Scaffold Driven by Colloidal Aggregation.Chembiochem : a European journal of chemical biology · 2026Article
- Synthesis, crystal structure and Hirshfeld surface analysis of 2-oxo-Acta crystallographica. Section E, Crystallographic communications · 2026Article
- Reply to: "The non-cytotoxic small molecule NPB does not inhibit BAD phosphorylation and forms colloidal aggregates".Communications medicine · 2025Article
- The non-cytotoxic small molecule NPB does not inhibit BAD phosphorylation and forms colloidal aggregates.Communications medicine · 2025Article
- Non-apoptotic cell death induction via sapogenin based supramolecular particles.Scientific reports · 2022Article
- Sequence-independent recognition of the amyloid structural motif by GFP protein family.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- A new era for understanding amyloid structures and disease.Nature reviews. Molecular cell biology · 2018Review
- Enzymatic Self-Assembly Confers Exceptionally Strong Synergism with NF-κB Targeting for Selective Necroptosis of Cancer Cells.Journal of the American Chemical Society · 2018Article
- An in situ Dynamic Continuum of Supramolecular Phosphoglycopeptides Enables Formation of 3D Cell Spheroids.Angewandte Chemie (International ed. in English) · 2017Article
- Allosteric sensitization of proapoptotic BAX.Nature chemical biology · 2017Article
- Selectively Inducing Cancer Cell Death by Intracellular Enzyme-Instructed Self-Assembly (EISA) of Dipeptide Derivatives.Advanced healthcare materials · 2017Article
- Elucidating drug targets and mechanisms of action by genetic screens in mammalian cells.Chemical communications (Cambridge, England) · 2017Review
- Mitochondria localization induced self-assembly of peptide amphiphiles for cellular dysfunction.Nature communications · 2017Article
- Enzyme-Instructed Assembly and Disassembly Processes for Targeting Downregulation in Cancer Cells.Journal of the American Chemical Society · 2017Article
- Phosphorylation at SerThe Journal of biological chemistry · 2017Article
- Internal Structure and Preferential Protein Binding of Colloidal Aggregates.ACS chemical biology · 2017Article
- Crystal structures of three 6-substituted coumarin-3-carboxamide derivatives.Acta crystallographica. Section E, Crystallographic communications · 2016Article
- Enzyme-Instructed Self-Assembly of Small D-Peptides as a Multiple-Step Process for Selectively Killing Cancer Cells.Journal of the American Chemical Society · 2016Article
- α-Synuclein and huntingtin exon 1 amyloid fibrils bind laterally to the cellular membrane.Scientific reports · 2016Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
We previously discovered a small-molecule inducer of cell death, named 1541, that noncovalently self-assembles into chemical fibrils ('chemi-fibrils') and activates procaspase-3 in vitro. We report here that 1541-induced cell death is caused by the fibrillar rather than the soluble form of the drug. A short hairpin RNA screen reveals that knockdown of genes involved in endocytosis, vesicle trafficking and lysosomal acidification causes partial 1541 resistance. We confirm the role of these pathways using pharmacological inhibitors. Microscopy shows that the fluorescent chemi-fibrils accumulate in punctae inside cells that partially colocalize with lysosomes. Notably, the chemi-fibrils bind and induce liposome leakage in vitro, suggesting they may do the same in cells. The chemi-fibrils induce extensive proteolysis including caspase substrates, yet modulatory profiling reveals that chemi-fibrils form a distinct class from existing inducers of cell death. The chemi-fibrils share similarities with proteinaceous fibrils and may provide insight into their mechanism of cellular toxicity.
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