ArticleJournal of medicinal chemistry2021
Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting.
Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
- PCFT-Independent Cellular Uptake of Cyclic Cell-Penetrating Peptide-Conjugated Folic Acid.Chembiochem : a European journal of chemical biology · 2025Article
- In silico study of active delivery of a photodynamic therapy drug targeting the folate receptor.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2025Article
- Harnessing Extracellular Vesicles for Targeted Drug Delivery in Ovarian Cancer.Pharmaceutics · 2025Review
- Identification of Innovative Folate Inhibitors Leveraging the Amino Dihydrotriazine Motif from Cycloguanil for Their Potential as Anti-ACS infectious diseases · 2024Article
- Package delivered: folate receptor-mediated transporters in cancer therapy and diagnosis.Chemical science · 2024Review
- Enhanced anticancer effect of thymidylate synthase dimer disrupters by promoting intracellular accumulation.Frontiers in pharmacology · 2024Article
- pH-responsive bond as a linker for the release of chemical drugs from RNA-drug complexes in endosome or lysosome.RNA nanomed · 2024Article
- Polymeric biomaterial-inspired cell surface modulation for the development of novel anticancer therapeutics.Biomaterials research · 2023Review
- Abiotic peptides as carriers of information for the encoding of small-molecule library synthesis.Science (New York, N.Y.) · 2023Article
- Serum Mass Spectrometry Proteomics and Protein Set Identification in Response to FOLFOX-4 in Drug-Resistant Ovarian Carcinoma.Cancers · 2023Article
- Carborane-Containing Folic AcidInternational journal of molecular sciences · 2022Article
- Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides.Biomolecules · 2022Article
- Interfacial Peptides as Affinity Modulating Agents of Protein-Protein Interactions.Biomolecules · 2022Review
- A Novel Method of Magnetic Nanoparticles Functionalized with Anti-Folate Receptor Antibody and Methotrexate for Antibody Mediated Targeted Drug Delivery.Molecules (Basel, Switzerland) · 2022Article
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Authors and funding
17 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drug-target interaction, cellular internalization, and target engagement should be addressed to design a lead with high chances of success in further optimization stages. Accordingly, we have designed conjugates of folic acid with anticancer peptides able to bind human thymidylate synthase (hTS) and enter cancer cells through folate receptor α (FRα) highly expressed by several cancer cells. Mechanistic analyses and molecular modeling simulations have shown that these conjugates bind the hTS monomer-monomer interface with affinities over 20 times larger than the enzyme active site. When tested on several cancer cell models, these conjugates exhibited FRα selectivity at nanomolar concentrations. A similar selectivity was observed when the conjugates were delivered in synergistic or additive combinations with anticancer agents. At variance with 5-fluorouracil and other anticancer drugs that target the hTS catalytic pocket, these conjugates do not induce overexpression of this protein and can thus help combating drug resistance associated with high hTS levels.
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