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Pharmaceutics
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State of the Art of Membrane Active Peptides, 2nd Edition
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State of the Art of Membrane Active Peptides, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 30 August 2025 | Viewed by 4344

Special Issue Editors

Dr. Brînduşa Alina Petre

E-Mail Website
Guest Editor
1. Faculty of Chemistry, Al. I. Cuza University of Iasi, 11, Carol I Boulevard, 700506 Iasi, Romania
2. Department of Chemistry & Biomolecular Science, Clarkson University, 8 Clarkson Avenue, Potsdam, NY 13699, USA
3. Center for Fundamental Research and Experimental Development in Translation Medicine–TRANSCEND, Regional Institute of Oncology, 700483 Iasi, Romania
Interests: peptide chemistry; amyloid peptides; mass spectrometry; proteomics; enzymatic substrates; lysosomal rare diseases
Special Issues, Collections and Topics in MDPI journals
Dr. Corina Ciobanasu

E-Mail Website
Guest Editor
Institute for Physical and Theoretical Chemistry, Rheinische Friedrich-Wilhelms-University Bonn, Wegeler Str. 12, 53115 Bonn, Germany
Interests: cell penetrating peptides; antimicrobial peptides; fluorescence microscopy; molecular interactions; biomimetic systems; drug delivery systems
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to the Special Issue “State of the Art of Membrane Active Peptides, 2nd Edition”. This issue is focused on membrane-active peptides that interact with the cell membrane and exert their biological activity by delivering different molecules inside cells or by disrupting the membrane followed cell lysis. Cell-penetrating peptides (CPPs) surmount the membrane barrier and deliver a great number of cargoes into the cells. CPPs act by the direct translocation of the membrane, pore formation or by endocytic routes. Antimicrobial peptides (AMPs) are components of the innate immunity and serve as first line protection against pathogens. Nowadays, multidrug-resistant bacteria to available antibiotics represent a major challenge, and AMPs are used to create a new generation of antibacterial drugs. Antimicrobial peptides target the bacterial membrane and lyse it using different mechanisms, such as the toroidal pore, the carpet model or the barrel stave model. Membrane-active peptides are considered as promising alternatives to current pharmaceuticals. However, their therapeutic potential is restricted by the current understanding of their molecular mechanism of action.

This Special Issue aims to bring together the latest advances regarding the molecular mechanism of peptide internalization, techniques to reveal these modes of peptide uptake and develop new peptide sequences, biological activity, applications and clinical data.

In this Special Issue, original research articles and reviews are welcome. Research areas may include, but are not limited to, the following:

  • Molecular mechanisms of membrane-active peptides;
  • Techniques to reveal the molecular mechanisms of membrane-active peptides;
  • Recent advances in applications of membrane-active peptides in biotechnology and medicine;
  • New peptide sequences and their biological activity;
  • Drug delivery systems based on membrane-active peptides.

We look forward to receiving your contributions.

Dr. Brînduşa Alina Petre
Dr. Corina Ciobanasu
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • cell-penetrating peptides
  • antimicrobial peptides
  • homing peptides
  • drug delivery system
  • cellular internalization
  • nanoparticles
  • cellular targeting
  • therapeutics
  • diagnostics

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Related Special Issue

Published Papers (3 papers)

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Research

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23 pages, 3818 KiB  
Article
Enhancement of Antimicrobial Function by L/D-Lysine Substitution on a Novel Broad-Spectrum Antimicrobial Peptide, Phylloseptin-TO2: A Structure-Related Activity Research Study
by Weining Yin, Junting Yao, Xuwei Leng, Chengbang Ma, Xiaoling Chen, Yangyang Jiang, Tao Wang, Tianbao Chen, Chris Shaw, Mei Zhou and Lei Wang
Pharmaceutics 2024, 16(8), 1098; https://doi.org/10.3390/pharmaceutics16081098 - 21 Aug 2024
Cited by 1 | Viewed by 1468
Abstract
Antibiotic resistance poses a serious threat to public health globally, reducing the effectiveness of conventional antibiotics in treating bacterial infections. ESKAPE pathogens are a group of highly transmissible bacteria that mainly contribute to the spread of antibiotic resistance and cause significant morbidity and [...] Read more.
Antibiotic resistance poses a serious threat to public health globally, reducing the effectiveness of conventional antibiotics in treating bacterial infections. ESKAPE pathogens are a group of highly transmissible bacteria that mainly contribute to the spread of antibiotic resistance and cause significant morbidity and mortality in humans. Phylloseptins, a class of antimicrobial peptides (AMPs) derived from Phyllomedusidae frogs, have been proven to have antimicrobial activity via membrane interaction. However, their relatively high cytotoxicity and low stability limit the clinical development of these AMPs. This project aims to study the antimicrobial activity and mechanisms of a phylloseptin-like peptide, phylloseptin-TO2 (PSTO2), following rational amino acid modification. Here, PSTO2 (FLSLIPHAISAVSALAKHL-NH2), identified from the skin secretion of Phyllomedusa tomopterna, was used as the template for modification to enhance antimicrobial activity. Adding positive charges to PSTO2 through substitution with L-lysines enhanced the interaction of the peptides with cell membranes and improved their antimicrobial efficacy. The analogues SRD7 and SR2D10, which incorporated D-lysines, demonstrated significant antimicrobial effects against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) while also showing reduced haemolytic activity and cytotoxicity, resulting in a higher therapeutic index. Additionally, SRD7, modified with D-lysines, exhibited notable anti-proliferative properties against human lung cancer cell lines, including H838 and H460. This study thus provides a potential development model for new antibacterial and anti-cancer drugs combating antibiotic resistance. Full article
(This article belongs to the Special Issue State of the Art of Membrane Active Peptides, 2nd Edition)
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Review

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24 pages, 2668 KiB  
Review
Biosimilars Targeting Pathogens: A Comprehensive Review of Their Role in Bacterial, Fungal, Parasitic, and Viral Infections
by Mohamed Halawa, Ramez M. Rashad ElSayed, Tope Aderibigbe, Precious M. Newman, Briana E. Reid and Valerie J. Carabetta
Pharmaceutics 2025, 17(5), 581; https://doi.org/10.3390/pharmaceutics17050581 - 28 Apr 2025
Viewed by 451
Abstract
Biosimilars represent medicinal products that exhibit a high degree of similarity to an already sanctioned reference biologic agent, with negligible clinically significant disparities concerning safety, purity, or potency. These therapeutic modalities are formulated as economically viable substitutes for established biologics, thereby facilitating increased [...] Read more.
Biosimilars represent medicinal products that exhibit a high degree of similarity to an already sanctioned reference biologic agent, with negligible clinically significant disparities concerning safety, purity, or potency. These therapeutic modalities are formulated as economically viable substitutes for established biologics, thereby facilitating increased accessibility to sophisticated treatments for a range of medical conditions, including infectious diseases caused by bacterial, fungal, and viral pathogens. The current landscape of biosimilars includes therapeutic proteins, such as monoclonal antibodies, antimicrobial peptides, antiviral peptides, and antifungal peptides. Here, we discuss the obstacles inherent in the development of biosimilars, including the rapid mutation rates of pathogens. Furthermore, we discuss innovative technologies within the domain, including antibody engineering, synthetic biology, and cell-free protein synthesis, which exhibit potential for improving the potency and production efficiency of biosimilars. We end with a prospective outlook to highlight the importance and capacity of biosimilars to tackle emerging infectious diseases, highlighting the imperative need for ongoing research and financial commitment. Full article
(This article belongs to the Special Issue State of the Art of Membrane Active Peptides, 2nd Edition)
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25 pages, 1292 KiB  
Review
Designed Cell-Penetrating Peptide Constructs for Inhibition of Pathogenic Protein Self-Assembly
by Mona Kalmouni, Yujeong Oh, Wael Alata and Mazin Magzoub
Pharmaceutics 2024, 16(11), 1443; https://doi.org/10.3390/pharmaceutics16111443 - 12 Nov 2024
Viewed by 1732
Abstract
Peptides possess a number of pharmacologically desirable properties, including greater chemical diversity than other biomolecule classes and the ability to selectively bind to specific targets with high potency, as well as biocompatibility, biodegradability, and ease and low cost of production. Consequently, there has [...] Read more.
Peptides possess a number of pharmacologically desirable properties, including greater chemical diversity than other biomolecule classes and the ability to selectively bind to specific targets with high potency, as well as biocompatibility, biodegradability, and ease and low cost of production. Consequently, there has been considerable interest in developing peptide-based therapeutics, including amyloid inhibitors. However, a major hindrance to the successful therapeutic application of peptides is their poor delivery to target tissues, cells or subcellular organelles. To overcome these issues, recent efforts have focused on engineering cell-penetrating peptide (CPP) antagonists of amyloidogenesis, which combine the attractive intrinsic properties of peptides with potent therapeutic effects (i.e., inhibition of amyloid formation and the associated cytotoxicity) and highly efficient delivery (to target tissue, cells, and organelles). This review highlights some promising CPP constructs designed to target amyloid aggregation associated with a diverse range of disorders, including Alzheimer’s disease, transmissible spongiform encephalopathies (or prion diseases), Parkinson’s disease, and cancer. Full article
(This article belongs to the Special Issue State of the Art of Membrane Active Peptides, 2nd Edition)
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