ArticlePloS one2014
Side chain hydrophobicity modulates therapeutic activity and membrane selectivity of antimicrobial peptide mastoparan-X.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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The trial behind it
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Who cites it
31 citing papers in PubMed, 68 citations in OpenAlex.
- Antimelanoma Activity of the Mastoparan Peptides MPX and MP1: Cellular Selectivity and Mechanism of Action.Molecular pharmaceutics · 2026Article
- Implicit membrane for helical peptide selectivity toward bacterial membranes.Biophysical journal · 2026Article
- Structure-Antimicrobial Activity Relationships of Recombinant Host Defence Peptides Against Drug-Resistant Bacteria.Microbial biotechnology · 2025Article
- Oral administration of antimicrobial peptide MPX can effectively regulate LPS-mediated testicular oxidative stress and blood‒testis barrier damage.Scientific reports · 2025Article
- Synthesis, Antimalarial Activity and Molecular Dynamics Studies of Pipecolisporin: A Novel Cyclic Hexapeptide with Potent Therapeutic Potential.Molecules (Basel, Switzerland) · 2025Article
- Studies on the antibacterial activity of the antimicrobial peptide Mastoparan X against methicillin-resistantFrontiers in cellular and infection microbiology · 2025Article
- Antimicrobial and antioxidant activities of peptide derived from turmeric plant (Curcuma longa L).PloS one · 2024Article
- Article
- Comprehensive Insights into Medicinal Research on Imidazole-Based Supramolecular Complexes.Pharmaceutics · 2023Review
- Effects of the Antimicrobial Peptide Mastoparan X on the Performance, Permeability and Microbiota Populations of Broiler Chickens.Animals : an open access journal from MDPI · 2022Article
- Structure-Activity Relationship of New Chimeric Analogs of Mastoparan from the Wasp VenomInternational journal of molecular sciences · 2022Article
- Bioactive Peptides and Proteins from Wasp Venoms.Biomolecules · 2022Review
- Stings on wings: Proteotranscriptomic and biochemical profiling of the lesser banded hornet (Frontiers in molecular biosciences · 2022Article
- Bioactive peptides from venoms against glioma progression.Frontiers in oncology · 2022Review
- Wasp Venom Biochemical Components and Their Potential in Biological Applications and Nanotechnological Interventions.Toxins · 2021Review
- Characteristics and therapeutic applications of antimicrobial peptides.Biophysics reviews · 2021Review
- The Antimicrobial Peptide Mastoparan X Protects Against EnterohemorrhagicFrontiers in microbiology · 2021Article
- Effect of Hydrophobicity on the Anticancer Activity of Fatty-Acyl-Conjugated CM4 in Breast Cancer Cells.ACS omega · 2020Article
- Venom peptides in association with standard drugs: a novel strategy for combating antibiotic resistance - an overview.The journal of venomous animals and toxins including tropical diseases · 2020Review
- Antimicrobial Peptides as Anti-Infective Agents in Pre-Post-Antibiotic Era?International journal of molecular sciences · 2019Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The discovery of new anti-infective compounds is stagnating and multi-resistant bacteria continue to emerge, threatening to end the "antibiotic era". Antimicrobial peptides (AMPs) and lipo-peptides such as daptomycin offer themselves as a new potential class of antibiotics; however, further optimization is needed if AMPs are to find broad use as antibiotics. In the present work, eight analogues of mastoparan-X (MPX) were investigated, having side chain modifications in position 1, 8 and 14 to modulate peptide hydrophobicity. The self-association properties of the peptides were characterized, and the peptide-membrane interactions in model membranes were compared with the bactericidal and haemolytic properties. Alanine substitution at position 1 and 14 resulted in higher target selectivity (red blood cells versus bacteria), but also decreased bactericidal potency. For these analogues, the gain in target selectivity correlated to biophysical parameters showing an increased effective charge and reduction in the partitioning coefficient for membrane insertion. Introduction of an unnatural amino acid, with an octyl side chain by amino acid substitution, at positions 1, 8 and 14 resulted in increased bactericidal potency at the expense of radically reduced membrane target selectivity. Overall, optimized membrane selectivity or bactericidal potency was achieved by changes in side chain hydrophobicity of MPX. However, enhanced potency was achieved at the expense of selectivity and vice versa in all cases.
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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.