ArticleScientific reports2016
The rational search for selective anticancer derivatives of the peptide Trichogin GA IV: a multi-technique biophysical approach.
Article in Scientific reports, 2016. 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, 30 citations in OpenAlex.
- 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
- Exploring Peptaibol's Profile, Antifungal, and Antitumor Activity of Emericellipsin A ofMolecules (Basel, Switzerland) · 2022Article
- Water-Soluble Trichogin GA IV-Derived Peptaibols Protect Tomato Plants FromFrontiers in plant science · 2022Article
- Novel antimicrobial agents targeting theFrontiers in cellular and infection microbiology · 2022Review
- LyeTx I-b Peptide Attenuates Tumor Burden and Metastasis in a Mouse 4T1 Breast Cancer Model.Antibiotics (Basel, Switzerland) · 2021Article
- Analogs of a Natural Peptaibol Exert Anticancer Activity in Both Cisplatin- and Doxorubicin-Resistant Cells and in Multicellular Tumor Spheroids.International journal of molecular sciences · 2021Article
- The Emericellipsins A-E from an Alkalophilic FungusJournal of fungi (Basel, Switzerland) · 2021Article
- Transcriptomic and Ultrastructural Analyses ofFrontiers in microbiology · 2021Article
- Targeted Amino Acid Substitutions in aInternational journal of molecular sciences · 2020Article
- Systematic Quantification of Electron Transfer in a Bare Phospholipid Membrane Using Nitroxide-Labeled Stearic Acids: Distance Dependence, Kinetics, and Activation Parameters.Langmuir : the ACS journal of surfaces and colloids · 2020Article
- Rational Design of Antiangiogenic Helical Oligopeptides Targeting the Vascular Endothelial Growth Factor Receptors.Frontiers in chemistry · 2019Article
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peptaibols are peculiar peptides produced by fungi as weapons against other microorganisms. Previous studies showed that peptaibols are promising peptide-based drugs because they act against cell membranes rather than a specific target, thus lowering the possibility of the onset of multi-drug resistance, and they possess non-coded α-amino acid residues that confer proteolytic resistance. Trichogin GA IV (TG) is a short peptaibol displaying antimicrobial and cytotoxic activity. In the present work, we studied thirteen TG analogues, adopting a multidisciplinary approach. We showed that the cytotoxicity is tuneable by single amino-acids substitutions. Many analogues maintain the same level of non-selective cytotoxicity of TG and three analogues are completely non-toxic. Two promising lead compounds, characterized by the introduction of a positively charged unnatural amino-acid in the hydrophobic face of the helix, selectively kill T67 cancer cells without affecting healthy cells. To explain the determinants of the cytotoxicity, we investigated the structural parameters of the peptides, their cell-binding properties, cell localization, and dynamics in the membrane, as well as the cell membrane composition. We show that, while cytotoxicity is governed by the fine balance between the amphipathicity and hydrophobicity, the selectivity depends also on the expression of negatively charged phospholipids on the cell surface.
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