ArticleJournal of the American Chemical Society2011
Self-assembling small molecules form nanofibrils that bind procaspase-3 to promote activation.
Article in Journal of the American Chemical Society, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
36 citing papers in PubMed, 78 citations in OpenAlex.
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- Regulation of Peptidase Activity beyond the Active Site in Human Health and Disease.International journal of molecular sciences · 2023Review
- Regarding the Mechanisms of Promiscuous Cannabinoid Pharmacology: An Elephant Has Entered the Room.Cannabis and cannabinoid research · 2021Article
- Biological functions of supramolecular assemblies of small molecules in cellular environment.RSC chemical biology · 2021Article
- A supramolecular protein chaperone for vaccine delivery.Theranostics · 2020Article
- Down-regulating Proteolysis to Enhance Anticancer Activity of Peptide Nanofibers.Chemistry, an Asian journal · 2018Article
- Selectively Inducing Cancer Cell Death by Intracellular Enzyme-Instructed Self-Assembly (EISA) of Dipeptide Derivatives.Advanced healthcare materials · 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
- Derivatives of Procaspase-Activating Compound 1 (PAC-1) and their Anticancer Activities.Current medicinal chemistry · 2016Article
- Supramolecular Hydrogelators and Hydrogels: From Soft Matter to Molecular Biomaterials.Chemical reviews · 2015Review
- Enzyme-Instructed Intracellular Molecular Self-Assembly to Boost Activity of Cisplatin against Drug-Resistant Ovarian Cancer Cells.Angewandte Chemie (International ed. in English) · 2015Article
- Post-HTS case report and structural alert: Promiscuous 4-aroyl-1,5-disubstituted-3-hydroxy-2H-pyrrol-2-one actives verified by ALARM NMR.Bioorganic & medicinal chemistry letters · 2015Article
- Nanoscale Assemblies of Small Molecules Control the Fate of Cells.Nano today · 2015Article
- Supramolecular Detoxification of Neurotoxic Nanofibrils of Small Molecules via Morphological Switch.Bioconjugate chemistry · 2015Article
- Enzyme-instructed self-assembly: a multistep process for potential cancer therapy.Bioconjugate chemistry · 2015Review
- Mixing biomimetic heterodimers of nucleopeptides to generate biocompatible and biostable supramolecular hydrogels.Angewandte Chemie (International ed. in English) · 2015Article
- Enzyme transformation to modulate the ligand-receptor interactions between small molecules.Chemical communications (Cambridge, England) · 2015Article
- Ligand-receptor interaction catalyzes the aggregation of small molecules to induce cell necroptosis.Journal of the American Chemical Society · 2015Article
- Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Modulating enzyme function with small-molecule activators, as opposed to inhibitors, offers new opportunities for drug discovery and allosteric regulation. We previously identified a compound, called 1541, from a high-throughput screen (HTS) that stimulates activation of a proenzyme, procaspase-3, to generate mature caspase-3. Here we further investigate the mechanism of activation and report the surprising finding that 1541 self-assembles into nanofibrils exceeding 1 μm in length. These particles are an unanticipated outcome from an HTS that have properties distinct from standard globular protein aggregators. Moreover, 1541 nanofibrils function as a unique biocatalytic material that activates procaspase-3 via induced proximity. These studies demonstrate a novel approach for proenzyme activation through binding to fibrils, which may mimic how procaspases are naturally processed on protein scaffolds.
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What OpenQuestion holds
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.