ArticleAntimicrobial agents and chemotherapy2016
Single Amino Acid Substitutions at Specific Positions of the Heptad Repeat Sequence of Piscidin-1 Yielded Novel Analogs That Show Low Cytotoxicity and In Vitro and In Vivo Antiendotoxin Activity.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 38 citations in OpenAlex.
- Marine-derived Peptides As Anti-biofilm and Anti-virulence Agents: Mechanistic Insights and Applications Against Microbial Pathogens.Probiotics and antimicrobial proteins · 2026Review
- Analysis of In Silico Properties and In Vitro Immunomodulatory Effects of Seven Synthetic Host Defence Peptides in Gilthead Seabream (Sparus aurata) Leucocytes.Marine biotechnology (New York, N.Y.) · 2025Article
- The Overlapping Biology of Sepsis and Cancer and Therapeutic Implications.Biomedicines · 2025Review
- Innovative Strategies and Methodologies in Antimicrobial Peptide Design.Journal of functional biomaterials · 2024Review
- Enhancing Antimicrobial Peptide Activity through Modifications of Charge, Hydrophobicity, and Structure.International journal of molecular sciences · 2024Review
- Recent Advances in Antimicrobial Peptide Hydrogels.International journal of molecular sciences · 2023Review
- A trimeric coiled-coil motif binds bacterial lipopolysaccharides with picomolar affinity.Frontiers in cellular and infection microbiology · 2023Article
- An optimized antimicrobial peptide analog acts as an antibiotic adjuvant to reverse methicillin-resistant Staphylococcus aureus.NPJ science of food · 2022Article
- Role of Anti-Cancer Peptides as Immunomodulatory Agents: Potential and Design Strategy.Pharmaceutics · 2022Review
- Traditional and Computational Screening of Non-Toxic Peptides and Approaches to Improving Selectivity.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Switching Bond: Generation of New Antimicrobial Peptides via the Incorporation of an Intramolecular Isopeptide Bond.ACS infectious diseases · 2021Article
- Design, Engineering and Discovery of Novel α-Helical and β-Boomerang Antimicrobial Peptides against Drug Resistant Bacteria.International journal of molecular sciences · 2020Review
- High Cell Selectivity and Bactericidal Mechanism of Symmetric Peptides Centered on d-Pro-Gly Pairs.International journal of molecular sciences · 2020Article
- Antiviral activity of Piscidin 1 against pseudorabies virus both in vitro and in vivo.Virology journal · 2019Article
- Substitution of lysine for isoleucine at the center of the nonpolar face of the antimicrobial peptide, piscidin-1, leads to an increase in the rapidity of bactericidal activity and a reduction in toxicity.Infection and drug resistance · 2019Article
- Identification and Characterization of Novel Antimicrobial Peptide from Hippocampus comes by In Silico and Experimental Studies.Marine biotechnology (New York, N.Y.) · 2018Article
- Recent Advances in Antibacterial and Antiendotoxic Peptides or Proteins from Marine Resources.Marine drugs · 2018Review
- Identification of novel antimicrobial peptide from Asian sea bass (Lates calcarifer) by in silico and activity characterization.PloS one · 2018Article
- Comparative Pharmacokinetics and Preliminary Pharmacodynamics Evaluation of Piscidin 1 Against PRV and PEDV in Rats.Frontiers in chemistry · 2018Article
- Piscidin-1-analogs with double L- and D-lysine residues exhibited different conformations in lipopolysaccharide but comparable anti-endotoxin activities.Scientific reports · 2017Article
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Piscidin-1 possesses significant antimicrobial and cytotoxic activities. To recognize the primary amino acid sequence(s) in piscidin-1 that could be important for its biological activity, a long heptad repeat sequence located in the region from amino acids 2 to 19 was identified. To comprehend the possible role of this motif, six analogs of piscidin-1 were designed by selectively replacing a single isoleucine residue at a d (5th) position or at an a (9th or 16th) position with either an alanine or a valine residue. Two more analogs, namely, I5F,F6A-piscidin-1 and V12I-piscidin-1, were designed for investigating the effect of interchanging an alanine residue at a d position with an adjacent phenylalanine residue and replacing a valine residue with an isoleucine residue at another d position of the heptad repeat of piscidin-1, respectively. Single alanine-substituted analogs exhibited significantly reduced cytotoxicity against mammalian cells compared with that of piscidin-1 but appreciably retained the antibacterial and antiendotoxin activities of piscidin-1. All the single valine-substituted piscidin-1 analogs and I5F,F6A-piscidin-1 showed cytotoxicity greater than that of the corresponding alanine-substituted analogs, antibacterial activity marginally greater than or similar to that of the corresponding alanine-substituted analogs, and also antiendotoxin activity superior to that of the corresponding alanine-substituted analogs. Interestingly, among these peptides, V12I-piscidin-1 showed the highest cytotoxicity and antibacterial and antiendotoxin activities. Lipopolysaccharide (12 mg/kg of body weight)-treated mice, further treated with I16A-piscidin-1, the piscidin-1 analog with the highest therapeutic index, at a single dose of 1 or 2 mg/kg of body weight, showed 80 and 100% survival, respectively. Structural and functional characterization of these peptides revealed the basis of their biological activity and demonstrated that nontoxic piscidin-1 analogs with significant antimicrobial and antiendotoxin activities can be designed by incorporating single alanine substitutions in the piscidin-1 heptad repeat.
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