ArticleJACS Au2022
In Situ Synthesis of an Anticancer Peptide Amphiphile Using Tyrosine Kinase Overexpressed in Cancer Cells.
Article in JACS Au, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The trial behind it
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
9 citing papers in PubMed.
- Structure-Activity Relationship of Cycling Molecular Assemblies for Golgi Targeting and Disruption.Journal of medicinal chemistry · 2026Article
- Cryo-Structural Insights into Enzymatic Peptide Self-Assembly Driving Extrinsic Lytic Cell Death.Journal of the American Chemical Society · 2026Article
- Enzymatic self-assembly of short peptides for cell spheroid formation.Journal of materials chemistry. B · 2024Article
- Single molecule tracking based drug screening.Nature communications · 2024Article
- Enzymatic control of intermolecular interactions for generating synthetic nanoarchitectures in cellular environment.Science and technology of advanced materials · 2024Review
- Enzyme-Instructed Intracellular Peptide Assemblies.Accounts of chemical research · 2023Article
- Peptide Assemblies for Cancer Therapy.ChemMedChem · 2023Review
- An Exploration of Multiple Component Peptide Assemblies by Enzyme-Instructed Self-Assembly.ChemSystemsChem · 2023Article
- Role of Anti-Cancer Peptides as Immunomodulatory Agents: Potential and Design Strategy.Pharmaceutics · 2022Review
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cell-selective killing using molecular self-assemblies is an emerging concept for cancer therapy. Reported molecular self-assemblies are triggered by hydrolysis of well-designed molecules inside or outside cancer cells. This hydrolysis can occur in cancer and normal cells because of the abundance of water in living systems. Here, we report the in situ synthesis of a self-assembling molecule using a tyrosine kinase overexpressed in cancer cells. We designed a tyrosine-containing peptide amphiphile (C16-E4Y) that is transformed into a phosphorylated peptide amphiphile (C16-E4pY) by the overexpressed tyrosine kinase. Phosphorylation of C16-E4Y promoted self-assembly to form nanofibers in cancer cells. C16-E4Y exhibited selective cytotoxicity toward cancer cells overexpressing the tyrosine kinase. Self-assembled C16-E4pY induced endoplasmic reticulum stress that caused apoptotic cell death. Animal experiments revealed that C16-E4Y has antitumor activity. These results show that an enzyme overexpressed in cancer cells is available for intracellular synthesis of an antitumor self-assembling drug that is cell-selective.
Identifiers
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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.