ArticleInternational journal of molecular sciences2021
Analogs of a Natural Peptaibol Exert Anticancer Activity in Both Cisplatin- and Doxorubicin-Resistant Cells and in Multicellular Tumor Spheroids.
Article in International journal of molecular sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 22 citations in OpenAlex.
- Immobilized acyl-transfer molecular reactors enable the solid-phase synthesis of sterically hindered peptides.Nature chemistry · 2025Article
- Agar Composition Modulates Production of Trichoderma Peptaibols, Affecting Antibacterial and Antiproliferative Activity.Current microbiology · 2025Article
- Process Mass Intensity (PMI): A Holistic Analysis of Current Peptide Manufacturing Processes Informs Sustainability in Peptide Synthesis.The Journal of organic chemistry · 2024Review
- Special Issue "Peptides for Health Benefits 2021".International journal of molecular sciences · 2024Article
- Article
- Self-Assembly and Cytocompatibility of Amino Acid Conjugates Containing a Novel Water-Soluble Aromatic Protecting Group.Biomacromolecules · 2023Article
- Synthesis, Conformational Analysis and Antitumor Activity of the Naturally Occurring Antimicrobial Medium-Length Peptaibol Pentadecaibin and Spin-Labeled Analogs Thereof.International journal of molecular sciences · 2023Article
- Peptaibol Analogs Show Potent Antibacterial Activity against Multidrug Resistant Opportunistic Pathogens.International journal of molecular sciences · 2023Article
- Anticancer and Targeting Activity of Phytopharmaceutical Structural Analogs of a Natural Peptide fromInternational journal of molecular sciences · 2023Article
- Characterization of Peptaibols Produced by a Marine Strain of the FungusMetabolites · 2023Article
- Exploring Peptaibol's Profile, Antifungal, and Antitumor Activity of Emericellipsin A ofMolecules (Basel, Switzerland) · 2022Article
- Development of Breast Cancer Spheroids to Evaluate Cytotoxic Response to an Anticancer Peptide.Pharmaceutics · 2021Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Peptaibols, by disturbing the permeability of phospholipid membranes, can overcome anticancer drug resistance, but their natural hydrophobicity hampers their administration. By a green peptide synthesis protocol, we produced two water-soluble analogs of the peptaibol trichogin GA IV, termed K6-Lol and K6-NH2. To reduce production costs, we successfully explored the possibility of changing the naturally occurring 1,2-aminoalcohol leucinol to a C-terminal amide. Peptaibol activity was evaluated in ovarian cancer (OvCa) and Hodgkin lymphoma (HL) cell lines. Peptaibols exerted comparable cytotoxic effects in cancer cell lines that were sensitive-and had acquired resistance-to cisplatin and doxorubicin, as well as in the extrinsic-drug-resistant OvCa 3-dimensional spheroids. Peptaibols, rapidly taken up by tumor cells, deeply penetrated and killed OvCa-spheroids. They led to cell membrane permeabilization and phosphatidylserine exposure and were taken up faster by cancer cells than normal cells. They were resistant to proteolysis and maintained a stable helical structure in the presence of cancer cells. In conclusion, these promising results strongly point out the need for further preclinical evaluation of our peptaibols as new anticancer agents.
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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.