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Special Issue "Synthetic Peptides and Peptidomimetics: From Basic Science to Biomedical Applications"

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 30 June 2021.

Special Issue Editors

Dr. Nunzianna Doti
E-Mail Website
Guest Editor
Institute of Biostructures and Bioimaging (IBB)-CNR, Via Mezzocannone 16, 80134 Naples, Italy
Interests: drug design and development; peptide synthesis and characterization; targeting of protein-protein interaction involved in diseases, antibodies, neurodegeneration
Dr. Menotti Ruvo
E-Mail Website
Guest Editor
Institute of Biostructure and Bioimaging, National Research Council, via Mezzocannoe, 16, I-80134 Napoli, Italy
Interests: monoclonal antibodies; antibody functional fragments; antibody drug conjugates
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Special Issue Information

Dear colleagues,

Synthetic peptides are gaining increasing interest as both research tools in basic and applied science and as therapeutic and diagnostic agents in clinical settings. Their use as inhibitors of protein–protein interactions is becoming a common practice toward elucidating the binding mode of proteins, advancing our understanding of signaling cascades, and offering a viable contribution to the design and development of new drugs. Synthetic peptides are also ideal ligands for extracellular receptors, acting as potent activators of several cellular pathways such as those of the immune response. To date, about 60 peptides have been approved for human use worldwide, many of which are derived from natural molecules, and hundreds more are progressing through the different stages of clinical trials. However, the poor membrane permeability, short plasma half-life, and scarce oral bioavailability strongly limit their druggability and negatively impact on clinical aspects. In this scenario, novel structural modifications are continuously sought for improving pharmacokinetic properties. Among others, amino acid or backbone modifications and the introduction of non-natural amino acids and conjugation of chemical moieties that extend the half-life, improve cellular uptake, stabilize active conformations, and modulate solubility are constantly proposed. Given the high biocompatibility, generally low toxicity, and functionalization potential, peptides and peptidomimetics are also being increasingly employed to develop new functional biomaterials which are excellent cell culture substrates for medicinal applications or that may act as biorecognition elements for the detection of analytes such as proteins, nucleic acids, and pathogens. In this instance, peptides are also being used as recognition units for chip-based biosensors for clinical diagnosis.

We therefore invite academic and industrial investigators working in all these fields to submit original research articles or reviews describing and discussing the most recent advancements and developments in basic science and biomedical applications.

Potential topics include, but are not limited to:

  • Synthetic peptides and peptidomimetics as protein–protein inhibitors
  • Synthetic procedures for preparing peptides and peptidomimetics
  • Biochemical and biophysical characterization of peptides and peptidomimetics
  • Peptide-based bioconjugation
  • Nanoparticle-conjugated peptides
  • Peptide-based bioreceptors
  • Peptide-based biomaterials

Dr. Nunzianna Doti
Dr. Menotti Ruvo
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 papers will be 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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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.

Published Papers (1 paper)

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Open AccessArticle
Novel Cell Permeable Polymers of N-Substituted L-2,3-Diaminopropionic Acid (DAPEGs) and Cellular Consequences of Their Interactions with Nucleic Acids
Int. J. Mol. Sci. 2021, 22(5), 2571; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22052571 - 04 Mar 2021
Viewed by 376
The present study aimed to synthesize novel polycationic polymers composed of N-substituted L-2,3-diaminopropionic acid residues (DAPEGs) and investigate their cell permeability, cytotoxicity, and DNA-binding ability. The most efficient cell membrane-penetrating compounds (O2Oc-Dap(GO2)n-O2Oc-NH2, where n = 4, 6, and [...] Read more.
The present study aimed to synthesize novel polycationic polymers composed of N-substituted L-2,3-diaminopropionic acid residues (DAPEGs) and investigate their cell permeability, cytotoxicity, and DNA-binding ability. The most efficient cell membrane-penetrating compounds (O2Oc-Dap(GO2)n-O2Oc-NH2, where n = 4, 6, and 8) showed dsDNA binding with a binding constant in the micromolar range (0.3, 3.4, and 0.19 µM, respectively) and were not cytotoxic to HB2 and MDA-MB-231 cells. Selected compounds used in the transfection of a GFP plasmid showed high transfection efficacy and minimal cytotoxicity. Their interaction with plasmid DNA and the increasing length of the main chain of tested compounds strongly influenced the organization and shape of the flower-like nanostructures formed, which were unique for 5/6-FAM-O2Oc-[Dap(GO2)]8-O2Oc-NH2 and typical for large proteins. Full article
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